PIT

SKU: orb1704222

Description

PIT (2,2'-Pyridylisatogen tosylate) is a potent, non-competitive P2Y1 receptor antagonist (IC50=0.14 µM) that does not inhibit nucleotide binding. Its utility extends to in vitro and in vivo research on purinergic signaling in respiratory diseases, including studies related to chronic bronchitis and asthma pathophysiology.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 56583-49-4
• MW: 396.42
• Purity: 98.63% (May vary between batches)
• Formula: C₂₀H₁₆N₂O₅S
• SMILES: Cc1ccc(cc1)S(O)(=O)=O.[O-][N+]1=C(C(=O)c2ccccc12)c1ccccn1
• Target: P2Y Receptor
• Solubility: DMSO:75 mg/mL (189.19 mM);10% DMSO+90% Saline:3.3 mg/mL (8.32 mM);Ethanol:< 5.95 mg/mL

Bioactivity

• Target IC50:
  P2Y1:0.14 μM
• In Vivo:
  In mice with S-bromo-willardiine injection induced tonic and tonicoclonic seizures, intraperitoneal injection of PIT (10 mg/kg) prevents the white matter and the cortical plate lesions against the insult.
• In Vitro:
  PIT (100 nM-10 μM) diminishes human P2Y1 receptor signaling in a non-competitive and dose-dependent manner and dose-dependently blocks the agonist activity of 2-MeSADP. PIT (0.1-3 μM) increases ATP-responses 2-5 fold. PIT (3-100 μM) inhibits ATP-mediated inward current (IC50 = 13.2 μM). PIT shows affinity to adenosine receptor (pKi = 5.3).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

2,2'-Pyridylisatogen tosylate, 2,2'-Pyridylisatogen Tosylate, P2Y, P2Y Receptor, P2YReceptor, PIT

Compound Identifiers

PubChem CID

124333