solo per uso di ricerca
N. Cat.: S1985
| 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 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 551.14 | Formula | C10H14N5O13P3.2Na |
Conservazione (Dalla data di ricezione) | |
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| N. CAS | 987-65-5 | Scarica SDF | Conservazione delle soluzioni stock |
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| 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+] | ||
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In vitro |
Water : 100 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
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In vivo |
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Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
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.)
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.
| 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. |
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| 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 |
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(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 | -- |