PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist ofP2Y1 receptorwith anIC₅₀value of 0.14 μM for humanP2Y1 receptor. PIT antagonizesP2Y1 receptorsignaling 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^[1][2][3].

PIT (0.1-10 μM) non-competitively and dose-dependently diminishs human P2Y1 receptor signaling with an IC₅₀value of 0.14 μM^[1].
PIT (0.1-10 μM) completely blocks the agonist activity of 2-MeSADP^[1].
PIT (1 nM-10 μM) dose-dependently inhibits the accumulation of inositol phosphates induced by the agonist 2-MeSADP^[1].
PIT (1 nM-10 μM) dose-dependently blocks the P2Y1 receptor signaling induced by the endogenous agonist ADP^[1].
PIT (0.1-3 μM) increases ATP-responses 2-5 fold, while higher concentrations (3-100 μM) inhibits ATP-mediated inward current with an IC₅₀value of 13.2 μM^[2].
PIT shows a low affinity for a range of membrane receptors, including: α₁, α₂-adrenoceptors, 5-HT_1A, 5-HT_1B, 5-HT₂, 5-HT₃, D₁, D₂, muscarinic, central benzodiazepine, H₁, μ-opioid, dihydropyridine and batrachotoxin receptors with pK_ivalues of<5^[2].
PIT shows affinity to an adenosine (A₁) receptor with a pK_ivalue of 5.3^[2].
PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca^[2].

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^[3].

396.42

C₂₀H₁₆N₂O₅S

56583-49-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

DMSO : 83.33 mg/mL(210.21 mM;ultrasonic and warming and heat to 70℃)

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明