Home > Inhibitors & Agonists > GPCR > P2Y Receptor
Cat. No. Product name CAS No.
DC11209 ACT-246475

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

1159500-34-1
DC11210 ACT-281959

ACT-281959 (ACT281959) is the prodrug of ACT-246475, which is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

DC10618 BPTU

BPTU is an Allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM).

870544-59-5
DC7005 Cangrelor free acid

Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. It does not require metabolic conversion to an active metabolite. This allows cangrelor’s immediate effect after infusion, and the therapeutic effects can be maintained with continuous infusion.

163706-06-7
DC3147 Clopidogrel hydrogensulfate

Clopidogrel (Plavix) is an oral, thienopyridine class antiplatelet agent.

120202-66-6
DCAPI1417 Clopidogrel

Clopidogrel is an irreversible inhibitor of the P2Y12 receptor, which is responsible for initiating signal transduction via a GPCR. The signal cascade initiates platelet aggregation and thus clopidogrel has the effect of “thinning” the blood.

113665-84-2
DC7772 Elinogrel

Elinogrel is a reversible P2Y12 receptor antagonist for the treatment of acute coronary syndrome and prevention of secondary thrombotic events.

936500-94-6
DC7203 MRS 2578

MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.

711019-86-2
DC1101 Ticagrelor (Brilinta,AZD6140)

Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist, also inhibits CYP2C9 and 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.

274693-27-5
DC28244 NF546

NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells.

1006028-37-0
DC28245 NF157

NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).

104869-26-3
DC28262 PSB-1114 tetrasodium

PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors.

1657025-60-9
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