| Description | PIT (2,2'-Pyridylisatogen tosylate) is a specific and non-competitive antagonist of the Purinergic receptor P2Y1 with an IC50 of 0.14 μM for human P2Y1. PIT does not affect nucleotide binding and can be used in studies about chronic bronchitis and asthma. |
| In vitro | PIT（100 nM-10 μM）以一种非竞争性及剂量依赖性方式减弱了人类P2Y1受体的信号传导，并且还以剂量依赖的方式阻断了2-MeSADP[1]的激动剂活性。PIT（0.1-3 μM）将ATP反应增加2-5倍。PIT（3-100 μM）抑制ATP介导的内向电流（IC50 = 13.2 μM）。PIT对腺苷受体表现出亲和性（pKi = 5.3）[2]。 |
| In vivo | 在通过S-bromo-willardiine注射诱发的小鼠强直性和强直-阵挛性癫痫中，腹腔注射PIT（10 mg/kg）能够防止由此伤害引起的白质和皮质板损伤[3]。 |
| Target activity | P2Y1:0.14 μM |
| Synonyms | 2,2'-Pyridylisatogen tosylate |
| molecular weight | 396.42 |
| Molecular formula | C20H16N2O5S |
| CAS | 56583-49-4 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 75.0 mg/mL (189.2 mM), Sonication and heating to 70℃ are recommended. Ethanol: < 5.95 mg/mL |
| References | 1. Gao ZG, et al. 2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochem Pharmacol. 2004 Jul 15;68(2):231-7. 2. King BF, et al. Potentiation by 2,2'-pyridylisatogen tosylate of ATP-responses at a recombinant P2Y1 purinoceptor. Br J Pharmacol. 1996 Mar;117(6):1111-8. 3. Menton K, et al. Role of spin trapping and P2Y receptor antagonism in the neuroprotective effects of 2,2'-pyridylisatogen tosylate and related compounds. Eur J Pharmacol. 2002 May 24;444(1-2):53-60. |