PIT

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PIT (2,2'-Pyridylisatogen tosylate) 是 P2Y1 受体 的选择性和非竞争性拮抗剂，对人 P2Y1 受体的 IC50 值为 0.14 μM。PIT 在不影响核苷酸结合的情况下拮抗 P2Y1 受体信号。PIT 是一些平滑肌中代谢性嘌呤受体 (P2Y 家族) 对 ATP 反应的不可逆拮抗剂。PIT 可用于慢性支气管炎和哮喘的研究。

PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma.

PIT (0.1-10 μM) non-competitively and dose-dependently diminishs human P2Y1 receptor signaling with an IC50 value of 0.14 μM.PIT (0.1-10 μM) completely blocks the agonist activity of 2-MeSADP.PIT (1 nM-10 μM) dose-dependently inhibits the accumulation of inositol phosphates induced by the agonist 2-MeSADP.PIT (1 nM-10 μM) dose-dependently blocks the P2Y1 receptor signaling induced by the endogenous agonist ADP.PIT (0.1-3 μM) increases ATP-responses 2-5 fold, while higher concentrations (3-100 μM) inhibits ATP-mediated inward current with an IC50 value of 13.2 μM.PIT shows a low affinity for a range of membrane receptors, including: α1, α2-adrenoceptors, 5-HT1A, 5-HT1B, 5-HT2, 5-HT3, D1, D2, muscarinic, central benzodiazepine, H1, μ-opioid, dihydropyridine and batrachotoxin receptors with pKi values of <5.PIT shows affinity to an adenosine (A1) receptor with a pKi value of5.3.PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca.

PIT (10 mg/kg; i.p.; for 5 days) significantly protects both the white matter and the cortical plate lesions against the insult in mice with S-bromo-willardiine injection induced tonic and tonicoclonic seizures.

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GPCR/G Protein

P2Y Receptor

P2Y Receptor

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56583-49-4

396.42

C20H16N2O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (210.21 mM; 超声助溶 (<70°C)

Cc1ccc(cc1)S(O)(=O)=O.[O-][N+]1=C(C(=O)c2ccccc12)c1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years