P2 Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S3737 Cangrelor Tetrasodium Cangrelor (AR-C69931MX) is a potent, competitive P2Y12 receptor inhibitor that is administered by intravenous infusion and rapidly achieves near complete inhibition of ADP-induced platelet aggregation.
J Immunother Cancer, 2024, 12(11)e009805
J Thromb Haemost, 2023, S1538-7836(23)00082-X
Food Funct, 2021, 10.1039/d1fo00531f
S2855 MRS 2578 MRS2578 is a potent P2Y6 receptor antagonist with an IC50 of 37 nM, and exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.
Ann Med, 2022, 54(1):1616-1626
Sci Rep, 2021, 11(1):15129
S4637 Prasugrel Hydrochloride Prasugrel hydrochloride (Prasugrel HCl, LY640315, PCR 4099 Hydrochloride) is a piperazine derivative and platelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome.
J Immunother Cancer, 2024, 12(11)e009805
Oncol Lett, 2018, 15(5):6107-6114
S1984 Ticlopidine HCl Ticlopidine HCl is a P2 receptor inhibitor against ADP-induced platelet aggregation with an IC50 of ~2 μM.
J Immunother Cancer, 2024, 12(11)e009805
E7266 Aurintricarboxylic acid Aurintricarboxylic acid is a potent, selective allosteric antagonist of P2X1R and P2X3R, with IC50 of 8.6 nM and 72.9 nM, respectively. It also functions as an anti-influenza agent by inhibiting viral neuraminidase. This compound suppresses apoptosis and is a potent inhibitor of topoisomerase II with an ID50 of ~7 nM in relaxation assays.
E4929 (S)-Clopidogrel (S)-Clopidogrel is an inhibitor of P2Y12 and exerts anticoagulant effects. It is metabolised into an active form that binds to the P2Y12 receptor, blocking ADP and preventing platelet aggregation. It also exhibits anti-inflammatory and antifibrotic properties in chronic kidney disease (CKD) and liver fibrosis.
S0053 CAY10593 (VU0155069) CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation.
Free Radic Biol Med, 2021, S0891-5849(21)00821-2
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S3293 Gardenoside Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. It inhibits TNF-α, IL-1β, IL-6 and NFκB activation. This compound also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. It suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.