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PIT

Catalog No. T23164   CAS 56583-49-4
Synonyms: 2,2'-Pyridylisatogen tosylate

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.

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PIT Chemical Structure
PIT, CAS 56583-49-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 57.00
10 mg In stock $ 97.00
25 mg In stock $ 197.00
50 mg In stock $ 332.00
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Purity: 99.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 P2Y1:0.14 μM
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[1]. 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)[2].
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[3].
Synonyms 2,2'-Pyridylisatogen tosylate
Molecular Weight 396.42
Formula C20H16N2O5S
CAS No. 56583-49-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 75.0 mg/mL (189.2 mM), Sonication and heating to 70℃ are recommended.

Ethanol: < 5.95 mg/mL

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library GPCR Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

PIT 56583-49-4 GPCR/G Protein Neuroscience P2Y Receptor 2,2'-Pyridylisatogen tosylate 2,2'-Pyridylisatogen Tosylate inhibitor inhibit

 

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