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  • DC Chemicals Limited
  • China
  • Product Name: PIT
  • Price: ¥Inquiry/100mg ¥Inquiry/250mg ¥Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 10 Day
  • Contact: Tony Cao

56583-49-4

56583-49-4 structure
56583-49-4 structure
  • Name: PIT
  • Chemical Name: PIT,2-(2-Pyridinyl)-(3H)-indol-3-one-1-oxide4-methylbenzenesulfonate
  • CAS Number: 56583-49-4
  • Molecular Formula: C20H16N2O5S
  • Molecular Weight: 396.41600
  • Catalog: Signaling Pathways GPCR/G Protein P2Y Receptor
  • Create Date: 2016-10-05 11:53:19
  • Modify Date: 2024-01-06 19:43:21
  • 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[1][2][3].

Name PIT,2-(2-Pyridinyl)-(3H)-indol-3-one-1-oxide4-methylbenzenesulfonate
Synonyms 2,2'-pyridylisatogen tosylate
PIT
Description 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[1][2][3].
Related Catalog
Target

P2Y1 Receptor:0.14 μM μM (IC50)

In Vitro PIT (0.1-10 μM) non-competitively and dose-dependently diminishs human P2Y1 receptor signaling with an IC50 value 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 IC50 value of 13.2 μM[2]. 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[2]. PIT shows affinity to an adenosine (A1) receptor with a pKi value of 5.3[2]. PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca[2].
In Vivo 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].
Molecular Formula C20H16N2O5S
Molecular Weight 396.41600
Exact Mass 396.07800
PSA 121.46000
LogP 4.19030