An antagonist of the P2Y12 receptor
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AZD 1283

Item No. 27649

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-3-pyridinecarboxylic acid, ethyl ester
CAS Number
919351-41-0
Molecular Formula
C23H26N4O5S
Formula Weight
470.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:4): 0.20 mg/mlDMSO: 15 mg/ml
λmax
215, 296 nm
SMILES
CCOC(C1=CC(C#N)=C(N2CCC(C(NS(CC3=CC=CC=C3)(=O)=O)=O)CC2)N=C1C)=O
InChi Code
InChI=1S/C23H26N4O5S/c1-3-32-23(29)20-13-19(14-24)21(25-16(20)2)27-11-9-18(10-12-27)22(28)26-33(30,31)15-17-7-5-4-6-8-17/h4-8,13,18H,3,9-12,15H2,1-2H3,(H,26,28)
InChi Key
NEMHKCNXXRQYRF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $103

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    10 mg

    $186

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    25 mg

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    Product Description

    AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).1 It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.1,2 AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bach, P., Antonsson, T., Bylund, R., et al. Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. Separation of the antithrombotic effect and bleeding for candidate drug AZD1283. J. Med. Chem. 56(17), 7015-7024 (2013).

    2. Giordanetto, F., Bach, P., Zetterberg, F., et al. Optimization of ketone-based P2Y12 receptor antagonists as antithrombotic agents: Pharmacodynamics and receptor kinetics considerations. Bioorg. Med. Chem. Lett. 24(13), 2963-2968 (2014).