A P2Y1 receptor negative allosteric modulator
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PIT

Item No. 45579

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-oxide 2-(2-pyridinyl)-3H-indol-3-one, 4-methylbenzenesulfonate
CAS Number
56583-49-4
Synonyms
  • 2,2’-Pyridylisatogen tosylate
Molecular Formula
C13H8N2O2 • C7H8O3S
Formula Weight
396.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C2=C([N+]([O-])=C1C3=NC=CC=C3)C=CC=C2.O=S(O)(C4=CC=C(C)C=C4)=O
InChi Code
InChI=1S/C13H8N2O2.C7H8O3S/c16-13-9-5-1-2-7-11(9)15(17)12(13)10-6-3-4-8-14-10;1-6-2-4-7(5-3-6)11(8,9)10/h1-8H;2-5H,1H3,(H,8,9,10)
InChi Key
MMPTYEXNPWSTOR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $117

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    25 mg

    $244

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    50 mg

    $358

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    Product Description

    PIT is a negative allosteric modulator of the purinergic P2Y1 receptor.1 It selectively inhibits agonist-induced signaling for P2Y1 over P2Y2, P2Y4, and P2Y11 receptors in 1321N1 cells and the P2Y12 receptor in CHO cells at 10 µM. PIT inhibits ATP-induced relaxation of guinea pig taenia caeci preparations and reduces periventricular white matter and cortical plate lesions induced by S-bromo-willardiine in mice.2 PIT is also a spin trap that forms stable adducts with hydroxyl and superoxide radicals.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gao, Z.-G., Mamedova, L., Tchilibon, S., et al. 2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochem. Pharmacol. 68(2), 231-237 (2004).

    2. Menton, K., Spedding, M., Gressens, P., 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. 444(1-2), 53-60 (2002).

    3. Nepveu, F., Souchard, J.P., Rolland, Y., et al. 2-2'-Pyridylisatogen, a selective allosteric modulator of P2 receptors, is a spin trapping agent. Biochem. Biophys. Res. Commun. 242(2), 272-276 (1998).