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ATP disodium

N. Cat.: S1985

ATP disodium is a disodium salt form of adenosine-triphosphate which is a multifunctional nucleoside triphosphate.
ATP disodium Chemical Structure

Struttura chimica

Peso molecolare: 551.14

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.79%
99.79

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0301μM. 19419204
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0631μM. 19419204
1321N1 Function assay Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2, EC50=0.085μM. 11985476
1321N1 Function assay Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay, EC50=0.085μM. 19419868
1321N1 Function assay Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C, EC50=0.085μM. 17302398
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0958μM. 19419204
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.111μM. 19419204
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.12μM. 19419204
MDCK Function assay 10 uM Induction of intracellular calcium level in MDCK cells assessed as net peak value at 10 uM by Fura-2 in calcium free medium, Activity=0.132μM. 23163425
1321N1 Function assay 30 mins Agonist activity at GFP tagged-human P2Y1 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis, EC50=0.15μM. 21090681
NG108-15 Function assay Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin), EC50=0.18μM. 29254895
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.183μM. 19419204
HEK293 Function assay Agonist activity at P2Y1 receptor expressed in human HEK293 cells, EC50=0.2μM. 20175517
HEK293 Function assay Agonist activity at rat P2Y1R expressed in HEK293 cells assessed as release of intracellular calcium by fluorescence based assay, EC50=0.2μM. 22873688
CF/T43 Function assay Agonist activity at P2Y2 receptor in human CF/T43 cells, EC50=0.2μM. 29254895
BEA Function assay Agonist activity at P2Y2 receptor in BEA cells (unknown origin), EC50=0.2μM. 29254895
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.237μM. 19419204
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.239μM. 19419204
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.299μM. 19419204
HEK 293 Function assay Concentration required for calcium mobilization at rat purinergic 2Y1 receptor expressed in HEK 293 cells, EC50=0.59μM. 15317453
1321N1 Function assay Antagonistic activity at human recombinant P2Y4 receptor expressed in 1321N1 cells, Kb=0.708μM. 17302398
1321N1 Function assay Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay, EC50=0.85μM. 23751098
1321N1 Function assay 30 mins Agonist activity at human P2Y1 receptor expressed in human 1321N1 cells assessed as increase of intracellular calcium level after 30 mins using fura-2 AM by fluorescence assay, EC50=0.85μM. 24846781
1321N1 Function assay Agonist activity at GFP-tagged human P2Y1R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay, EC50=0.85μM. 26447940
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=1μM. 19419204
1321N1 Function assay 30 mins Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method, EC50=1μM. 23075067
Sf9 Function assay Binding affinity to wild type 6XHis-tagged human JAK2 JH2 domain (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay, Kd=1.3μM. 32329617
Sf9 Function assay Binding affinity to 6XHis-tagged human JAK2 JH2 domain V617F mutant (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay, Kd=1.3μM. 32329617
1321N1 Function assay Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor, EC50=1.5μM. 11985476
Sf9 Function assay Binding affinity to recombinant human biotinylated N-terminal GST-tagged autophosphorylated TAK1 (1 to 303 residues) fused with TAB1 (437 to 504 residues) expressed in baculovirus infected sf9 cells by SPR assay, Kd=2.8μM. 28109791
1321N1 Function assay 30 mins Agonist activity at GFP tagged-human P2Y11 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis, EC50=3.3μM. 21090681
1321N1 Function assay Agonist activity at human GFP-tagged P2Y11R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay, EC50=6.7μM. 23751098
1321N1 Function assay Agonist activity at GFP-tagged human P2Y11R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay, EC50=6.7μM. 26447940
1321N1 Function assay Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=11.7μM. 19419204
1321N1 Function assay Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 11, EC50=17.3μM. 11985476
1321N1 Function assay Antagonistic activity at human recombinant P2Y4 receptor expressed in 1321N1 cells 17302398
MDCK Function assay 10 uM Induction of intracellular calcium level in MDCK cells at 10 uM by Fura-2 in calcium free medium in presence of 10 uM U73343 inactive analogue of U73122 phospholipase C inhibitor 23163425
THLP1 Function assay Agonist activity at NLRP3 in human THLP1-null cells assessed as induction of LPS-induced IL-1beta secretion by HEK-Blue reporter cell based assay 28829599
HEK293 Function assay 1 uM Agonist activity at ALX/FPR2 (unknown origin) expressed in HEK293 cells co-expressing Galphaq assessed as induction of intracellular calcium accumulation at 1 uM by Fluo-4 dye based fluorescence spectrophotometric assay 30419493
HEK293 Function assay 1 uM Induction of intracellular calcium accumulation in HEK293 cells at 1 uM by Fluo-4 dye based fluorescence spectrophotometric assay 30419493
BL21(DE3) Function assay Activity of Bacillus subtilis N-terminal His-tagged ANT(6) expressed in Escherichia coli BL21(DE3) cells assessed as adenylated product by Michaelis-Menten kinetics ChEMBL
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 551.14 Formula

C10H14N5O13P3.2Na

Conservazione (Dalla data di ricezione)
N. CAS 987-65-5 Scarica SDF Conservazione delle soluzioni stock

Sinonimi Adenosine-Triphosphate disodium, Adenosine 5'-triphosphate Smiles C1=NC(=C2C(=N1)N(C=N2)C3C(C(C(O3)COP(=O)(O)OP(=O)([O-])OP(=O)(O)[O-])O)O)N.[Na+].[Na+]

Solubilità (Solubility)

In vitro
Lotto:

Water : 100 mg/mL

DMSO : Insoluble
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 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 l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è 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, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

In vitro

ATP release and autocrine feedback through P2Y2 and A3 receptors provide signal amplification, controlling gradient sensing and migration of neutrophils. ATP results in production of reactive oxygen species (ROS), which stimulates the phosphatidylinositol 3-kinase (PI3K) pathway and subsequent Akt and ERK1/2 activation. ATP-dependent ROS production and PI3K activation also stimulate transcription of genes required for an oxidative stress response. ATP-mediated ROS-dependent PI3K is required for activation of caspase-1 and secretion of IL-1beta and IL-18. ATP potently stimulates TNF-alpha release, resulting from TNF-alpha mRNA expression in rat cultured brain microglia. ATP-induced TNF-alpha release is Ca(2+)-dependent, and a sustained Ca(2+) influx correlated with the TNF-alpha release in ATP-stimulated microglia. ATP-induced TNF-alpha release is inhibited by PD 098059, an inhibitor of extracellular signal-regulated protein kinase (ERK) kinase 1 (MEK1), which activates ERK, and also by SB 203580, an inhibitor of p38 mitogen-activated protein kinase. ATP rapidly activates both ERK and p38 even in the absence of extracellular Ca(2+). ATP-induced cytotoxicity is mediated by classical alterations of apoptosis, including membrane blebbing, nuclear condensation, and DNA fragmentation. ATP but not other nucleotides lead to the potent and selective activation of NF-κB in microglial cells through a P2Z receptor-mediated pathway.

In vivo

ATP regulates microglial branch dynamics in the intact mice brain, and its release from the damaged tissue and surrounding astrocytes mediates a rapid microglial response towards injury.

Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/9412459/
  • [5] https://pubmed.ncbi.nlm.nih.gov/1589508/

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
NCT04760860 Not yet recruiting
Dementia With Lewy Bodies
Qiang Zhang|University of Iowa
October 2024 Phase 1|Phase 2
NCT05590195 Not yet recruiting
Bacterial Vaginosis|Bacterial Infections|Bacterial Vaginosis | Vaginal | Microbiology|Vaginal Infection
Jeremy Burton|Deerland Enzymes|Lawson Health Research Institute|St. Joseph''s Health Care London
May 1 2024 Phase 3
NCT06167512 Not yet recruiting
Multi-organ Failure After Severe Trauma
Assistance Publique - Hôpitaux de Paris
April 1 2024 --