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GSK269962A HCl ROCK inibitore

N. Cat.S7687

GSK269962A HCl è un inibitore selettivo di ROCK (Rho-associated protein kinase) con valori di IC50 di 1,6 e 4 nM per ROCK1 e ROCK2, rispettivamente.
GSK269962A HCl ROCK inibitore Chemical Structure

Struttura chimica

Peso molecolare: 607.06

Vai a

Controllo Qualità

Lotto: Purezza: 99.59%
99.59

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dellattività PMID
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=18.8477 μM
NCI-H1694 Growth inhibition assay Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=24.8749 μM
NCI-H1963 Growth inhibition assay Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50=1.27839 μM
NCI-H2081 Growth inhibition assay Inhibition of human NCI-H2081 cell growth in a cell viability assay, IC50=34.6044 μM
NCI-H209 Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=22.6272 μM
NCI-H2107 Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=25.6561 μM
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=6.50426 μM
NCI-H2171 Growth inhibition assay Inhibition of human NCI-H2171 cell growth in a cell viability assay, IC50=0.95937 μM
NCI-H2227 Growth inhibition assay Inhibition of human NCI-H2227 cell growth in a cell viability assay, IC50=7.88616 μM
NCI-H524 Growth inhibition assay Inhibition of human NCI-H524 cell growth in a cell viability assay, IC50=22.8763 μM
NCI-H526 Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=18.5431 μM
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=2.45161 μM
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=15.0578 μM
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.82294 μM
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=10.9496 μM
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=17.201 μM
ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.9191 μM
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=46.195 μM
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=8.71808 μM
P30-OHK cell Growth inhibition assay Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=7.62877 μM
P30-OHK cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=7.04954 μM
PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.22126 μM
QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=0.49004 μM
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=18.9036 μM
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=10.5662 μM
RL95-2 cell Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=10.67 μM
RPMI-6666 cell Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=18.5236 μM
RPMI-8402 cell Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=4.5856 μM
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.393 μM
Ramos-2G6-4C10 cell Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=1.357 μM
SCLC-21H cell Growth inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50=7.61149 μM
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=11.8321μM
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=6.23183 μM
SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=1.28661 μM
SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=5.75508 μM
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=11.7259 μM
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=1.04526 μM
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=32.5965 μM
SK-MM-2 cell Growth inhibition assay Inhibition of human SK-MM-2 cell growth in a cell viability assay, IC50=42.3405 μM
SK-N-DZ cell Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.48314 μM
SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=17.5456 μM
SK-PN-DW cell Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=24.9736 μM
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=8.07737 μM
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=0.000137 μM
SU-DHL-1 cell Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=12.7336 μM
SW684 cell Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50=39.011 μM
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.88656 μM
SW962 cell Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay, IC50=12.7521 μM
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.2991 μM
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.0793 μM
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=1.87034 μM
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=21.4387 μM
AM-38 cell Growth inhibition assay Inhibition of human AM-38 cell growth in a cell viability assay, IC50=7.26327 μM
ATN-1 cell Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=24.7555 μM
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=22.2532 μM
BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=0.00789 μM
human BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=3.97107 μM
BE-13 cell Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.14081μM
BL-70 cell Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=3.40703 μM
BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=18.8859 μM
Becker cell Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=13.9545 μM
CAL-148 cell Growth inhibition assay Inhibition of human CAL-148 cell growth in a cell viability assay, IC50=35.6557 μM
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50=22.8423 μM
TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=32.4114 μM
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=11.6089 μM
TE-9 cell Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=36.6381 μM
TGW cell Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50=23.3577 μM
UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=8.70625 μM
WSU-NHL cell Growth inhibition assay Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=27.1907 μM
no-10 cell Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50=0.66846 μM
no-11 cell Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50=47.0263 μM
CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=0.847 μM
CCRF-CEM cell Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=8.65392 μM
CMK cell Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50=1.01323 μM
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=3.24226 μM
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=2.0738 μM
CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=36.5497 μM
CRO-AP2 cell Growth inhibition assay Inhibition of human CRO-AP2 cell growth in a cell viability assay, IC50=2.36088 μM
CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=23.9145 μM
Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=47.586 μM
D-247MG cell Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=0.62814 μM
D-263MG cell Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay, IC50=0.08509 μM
D-336MG cell Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.62854 μM
D-392MG cell Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=1.43039 μM
D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=8.53492 μM
D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=12.3152 μM
DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=47.1417 μM
DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=7.01898 μM
DMS-114 cell Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=49.8468 μM
DMS-153 cell Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=42.9923 μM
DOHH-2 cell Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=4.22764 μM
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=8.43623 μM
Daudi cell Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=2.09802 μM
EC-GI-10 cell Growth inhibition assay Inhibition of human EC-GI-10 cell growth in a cell viability assay, IC50=44.2589 μM
ECC4 cell Growth inhibition assay Inhibition of human ECC4 cell growth in a cell viability assay, IC50=32.1896 μM
EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=2.45594 μM
ES1 cell Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=5.54087 μM
ES3 cell Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50=42.4729 μM
ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay, IC50=35.195 μM
ES6 cell Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=0.24733 μM
ES7 cell Growth inhibition assay Inhibition of human ES7 cell growth in a cell viability assay, IC50=5.23124 μM
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.81924 μM
EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=13.6759 μM
EW-22 cell Growth inhibition assay Inhibition of human EW-22 cell growth in a cell viability assay, IC50=47.7947 μM
GCIY cell Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay, IC50=9.80389 μM
GDM-1 cell Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=8.39196 μM
GI-1 cell Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=0.00523 μM
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=0.04951 μM
GR-ST cell Growth inhibition assay Inhibition of human GR-ST cell growth in a cell viability assay, IC50=13.7902 μM
GT3TKB cell Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50=1.60389 μM
HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=6.69712 μM
HCC1599 cell Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50=37.6011 μM
HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=13.3834 μM
HD-MY-Z cell Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=25.2146 μM
HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=12.2114 μM
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=23.9527 μM
HT cell Growth inhibition assay Inhibition of human HT cell growth in a cell viability assay, IC50=4.44321 μM
HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=4.90686 μM
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=3.78986 μM
IST-MEL1 cell Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=32.9086 μM
IST-SL1 cell Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=2.17079 μM
IST-SL2 cell Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=3.26608 μM
K052 cell Growth inhibition assay Inhibition of human K052 cell growth in a cell viability assay, IC50=0.75301 μM
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=33.5915 μM
KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=29.3969 μM
KARPAS-422 cell Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=42.9142 μM
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=4.11247 μM
KE-37 cell Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50=9.835 μM
KG-1 cell Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=23.9757 μM
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=0.56742 μM
KM12 cell Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=3.52964 μM
KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=30.4549 μM
KNS-42 cell Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay, IC50=8.81915 μM
KNS-81-FD cell Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50=37.426 μM
KS-1 cell Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.0046 μM
KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=23.484 μM
L-540 cell Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=20.7445 μM
LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=13.6742 μM
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=28.3883 μM
LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=10.5536 μM
LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=1.71496μM
LB831-BLC cell Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=11.1726 μM
LB996-RCC cell Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=12.7431 μM
LC4-1 cell Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50=32.8341 μM
LOUCY cell Growth inhibition assay Inhibition of human LOUCY cell growth in a cell viability assay, IC50=1.15276 μM
LOXIMVI cell Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.2122 μM
LS-123 cell Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=39.2258 μM
LU-134-A cell Growth inhibition assay Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=7.14068 μM
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=22.218 μM
LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=17.4351μM
MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50=45.0841 μM
MDA-MB-134-VI cell Growth inhibition assay Inhibition of human MDA-MB-134-VI cell growth in a cell viability assay, IC50=39.2486 μM
MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.64383 μM
MHH-NB-11 cell Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=0.0669 μM
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=3.40304 μM
MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=4.43653 μM
MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=4.11163 μM
MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=14.4124 μM
MPP-89 cell Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=1.25922 μM
MRK-nu-1 cell Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=0.57572 μM
MSTO-211H cell Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=12.869 μM
MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.13915 μM
NALM-6 cell Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=1.56109 μM
NB1 cell Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50=3.84369 μM
NB10 cell Growth inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50=0.13915 μM
NB12 cell Growth inhibition assay Inhibition of human NB12 cell growth in a cell viability assay, IC50=16.5656 μM
NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=2.31278 μM
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay, IC50=3.58051 μM
NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50=0.59114 μM
NCCIT cell Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50=41.8453 μM
NCI-H1155 cell Growth inhibition assay Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50=14.3408 μM
NCI-H1304 cell Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay, IC50=11.8982 μM
NCI-H1355 cell Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.9411 μM
NCI-H1395 cell Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=22.8795 μM
NCI-H1417 cell Growth inhibition assay Inhibition of human NCI-H1417 cell growth in a cell viability assay, IC50=5.67522 μM
NCI-H1436 cell Growth inhibition assay Inhibition of human NCI-H1436 cell growth in a cell viability assay, IC50=3.84101 μM
NTERA-S-cl-D1 cell Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=12.8935 μM
JiyoyeP-2003 cell Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=36.6284 μM
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Informazioni chimiche, conservazione e stabilità

Peso molecolare 607.06 Formula

C29H30N8O5.HCl

Conservazione (Dalla data di ricezione)
N. CAS 2095432-71-4 Scarica SDF Conservazione delle soluzioni stock

Sinonimi GSK269962B, GSK269962 Smiles CCN1C2=CC(=NC=C2N=C1C3=NON=C3N)OC4=CC=CC(=C4)NC(=O)C5=CC=C(C=C5)OCCN6CCOCC6.Cl

Solubilità

In vitro
Lotto:

DMSO : 100 mg/mL (164.72 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 28 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC50/Ki
ROCK1
(Cell-free assay)
1.6 nM
ROCK2
(Cell-free assay)
4 nM
MSK1
(Cell-free assay)
49 nM
RSK1
(Cell-free assay)
132 nM
In vitro
GSK269962A ha completamente abolito la formazione di fibre di stress actiniche indotta dall'angiotensina II nei muscoli lisci umani. Tale effetto soppressivo sulla formazione di fibre actiniche è stato osservato a partire da circa 1 μM di GSK269962A. GSK269962A ha indotto vasodilatazione in aorte di ratto pre-costrette (bagni tissutali) con una IC50 di 35 nM. La vasodilatazione indotta da GSK269962A è reversibile. GSK269962A ha soppresso la trascrizione dell'mRNA di IL-6 e ha ridotto la produzione di proteine IL-6 e TNF-α indotta da LPS nei macrofagi.
In vivo
La somministrazione orale di GSK269962A ha prodotto una profonda riduzione dose-dipendente della pressione sanguigna sistemica nei ratti spontaneamente ipertesi. La riduzione della pressione sanguigna è stata acuta e sostanziale. L'effetto massimo sulla pressione sanguigna è stato osservato circa 2 ore dopo la somministrazione orale. La riduzione della pressione sanguigna è stata accompagnata da un aumento acuto e dose-dipendente della frequenza cardiaca, presumibilmente dovuto all'attivazione del meccanismo baroriflesso. L'inibizione di ROCK con l'uso di GSK 269962 alla dose di 10 mg/kg, a sua volta, ha innescato un aumento di VV (volume svuotato), PVR (residuo post-svuotamento), VT (soglia di volume), VE (efficienza di svuotamento), ICI (intervallo di intercontrazione), BC (compliance vescicale) e VTNVC (soglia di volume per elicitare NVC). L'inibizione della via ROCK attraverso GSK 269962 non sembrava avere alcun effetto su HR (frequenza cardiaca), SBP (pressione sanguigna sistolica), MBP (pressione sanguigna sistolica) o DBP (pressione sanguigna diastolica). NVC:nonvoiding contractions.
Riferimenti

Supporto tecnico

Istruzioni per la manipolazione

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