P2Y Receptor

P2Y receptors are a family of purinergic G protein-coupled receptors, stimulated by nucleotides such as ATP, ADP, UTP, UDP and UDP-glucose. To date, 12 P2Y receptors have been cloned in humans: P2Y1, P2Y2, P2Y4, P2Y5, P2Y6, P2Y8, P2Y9, P2Y10, P2Y11, P2Y12, P2Y13 and P2Y14. P2Y receptors are present in almost all human tissues where they exert various biological functions based on their G-protein coupling. P2Y2 is a potential drug target for treating cystic fibrosis. P2Y11 is a regulator of immune response, and a common polymorphism carried by almost 20% of North European caucasians give increased risk of myocardial infarction, making P2Y11 an interesting drug target candidate for treatment of myocardial infarction. P2Y12 is the target of the anti-platelet drug clopidogrel and other thienopyridines.

www.MedChemExpress.com 1 P2Y Receptor Inhibitors, Agonists, Antagonists & Modulators

2-Methylthioadenosine diphosphate trisodium Adenosine 2',5'-diphosphate sodium (2-Methylthio-ADP trisodium) Cat. No.: HY-108648 Cat. No.: HY-N7740

2-Methylthioadenosine diphosphate trisodium is a Adenosine 2',5'-diphosphate sodium is a potent purinergic P2Y receptors agonist, with competitive P2Y1 antagonist. Adenosine

EC50s of 19, 6.2, and 5 nM for human P2Y13, 2',5'-diphosphate sodium exhibits non-selective mouse P2Y13 and human P2Y12, respectively. antagonism at recombinant and human platelet P2X1 receptors.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg

AZD1283 BPTU Cat. No.: HY-15799 (BMS-646786) Cat. No.: HY-13831

AZD1283 is a potent antagonist of the P2Y12 BPTU (BMS-646786) is a non-nucleotide P2Y1 receptor with EC50 of 3.0 ug/kg/min, TI >10; receptor allosteric antagonist with antithrombotic with binding IC50 of 11 nM. activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.

Purity: 99.11% Purity: 99.84% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Cangrelor tetrasodium Clopidogrel Cat. No.: HY-19638A Cat. No.: HY-15283

Cangrelor tetrasodium, an adenosine triphosphate Clopidogrel is an orally active platelet inhibitor analogue, is a reversible and selective platelet that targets P2Y12 receptor. Clopidogrel is used P2Y12 antagonist, with prompt and potent to inhibit blood clots in coronary artery disease, antiplatelet effects. peripheral vascular disease, and cerebrovascular disease.

Purity: 99.93% Purity: 99.57% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 100 mg

Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate; Clopidogrel thiolactone (S)-(+)-Clopidogrel hydrogen sulfate) Cat. No.: HY-17459 Cat. No.: HY-15876

Clopidogrel hydrogen sulfate is an antiplatelet Clopidogrel thiolactone is a P2Y12 receptor agent which works by blocking platelets from inhibitor, is a potent antiplatelet agent. sticking together and prevents them from forming harmful clots.

Purity: 99.67% Purity: >98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

Diquafosol tetrasodium Elinogrel (INS365) Cat. No.: HY-B0606 (PRT060128) Cat. No.: HY-11021

Diquafosol tetrasodium is a P2Y2 receptor agonist Elinogrel (PRT060128) is a potent, direct acting,

that stimulates fluid and mucin secretion on the competitive, and reversible platelet P2Y12

ocular surface, as a topical treatment of dry eye antagonist (IC50=20 nM). It is orally and disease. intravenously available and has potent antiplatelet effects.

Purity: 99.93% Purity: >98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

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MRS 2578 MRS2179 tetrasodium hydrate Cat. No.: HY-13104 Cat. No.: HY-101308A

MRS 2578 is a selective and potent P2Y6 receptor MRS2179 tetrasodium hydrate is a competitive P2Y1 antagonist with IC50s of 37 nM (human) and 98 nM receptor antagonist, with a Kb of 102 nM and a

(rat). MRS 2578 exhibits insignificant activity at pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 P2Y1, P2Y2, P2Y4, and P2Y11 receptors. tetrasodium hydrate is selective for P2Y1 over

P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. Purity: >98.0% Purity: >99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 5 mg

N6-(4-Hydroxybenzyl)adenosine NF157 (Para-topolin riboside) Cat. No.: HY-18775 Cat. No.: HY-108672

N6-(4-Hydroxybenzyl)adenosine is a inhibitor of NF157 is a highly selective nanomolar P2Y11 platelet aggregation induced in vitro by collagen antagonist with a pKi of 7.35. The IC50s are 463 and their activity range was demonstrated (IC50: nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1

6.77-141 μM). (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively.

Purity: 99.66% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Prasugrel Prasugrel (Maleic acid) (PCR 4099) Cat. No.: HY-15284 (PCR 4099 (Maleic acid)) Cat. No.: HY-15284B

Prasugrel (PCR 4099), a thienopyridine and Prasugrel (PCR 4099) Maleic acid is a prodrug, inhibits platelet function. Prasugrel is thienopyridine and prodrug, inhibits platelet an orally active and potent P2Y12 receptor function. Prasugrel Maleic acid is an orally antagonist, and inhibits ADP-induced platelet active and potent P2Y12 receptor antagonist, and aggregation. inhibits ADP-induced platelet aggregation.

Purity: >98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 1 mg, 5 mg

Prasugrel hydrochloride TAK-024 (PCR 4099 hydrochloride) Cat. No.: HY-15284A Cat. No.: HY-100254

Prasugrel hydrochloride (PCR 4099 hydrochloride), TAK-024 is a platelet inhibitor with IC50s of 31, a thienopyridine and prodrug, inhibits platelet 79 and 51 nM in human, monkey and guinea pig, function. Prasugrel hydrochloride is an orally respectively. active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.

Purity: 99.57% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

Ticagrelor trans-R-138727MP (AZD6140; AR-C 126532XX) Cat. No.: HY-10064 (Prasugrel metabolite R-138727MP) Cat. No.: HY-136588

Ticagrelor (AZD6140) is a reversible oral P2Y12 trans-R-138727MP (Prasugrel metabolite R-138727MP) receptor antagonist for the treatment of platelet is the active metabolite derivative of aggregation. Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function.

Purity: 99.88% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

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Uridine 5'-diphosphate sodium salt Uridine 5′-diphosphoglucose disodium salt Cat. No.: HY-W010820 (UDP-D-Glucose disodium salt) Cat. No.: HY-N7032

Uridine 5'-diphosphate sodium salt is a potent, Uridine 5′-diphosphoglucose disodium salt

selective P2Y6 receptor native agonist (UDP-D-Glucose disodium salt) is the precursor of

(EC50=300 nM; pEC50=6.52) and a potent P2Y14 glucose-containing oligosaccharides,

antagonist (pEC50=7.28). polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms.

Purity: >98% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Uridine diphosphate glucose Uridine-5'-diphosphate disodium salt Cat. No.: HY-113044 Cat. No.: HY-W010832

Uridine diphosphate glucose is the precursor of Uridine-5'-diphosphate disodium salt is a potent,

glucose-containing oligosaccharides, selective P2Y6 receptor native agonist

polysaccharides, glycoproteins, and glycolipids in (EC50=300 nM; pEC50=6.52) and a potent P2Y14

animal tissues and in some microorganisms. Uridine antagonist (pEC50=7.28).

diphosphate glucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR1.. Purity: >98% Purity: 98.01% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Vicagrel YM-254890 Cat. No.: HY-118284 Cat. No.: HY-111557

Vicagrel, an acetate derivative of Clopidogrel, is YM-254890 is a selective Gαq/11 protein inhibitor a P2Y12 platelet inhibitor potentially for the isolated from Chromobacterium sp. YM-254890 treatment of thrombosis, the substrate of shows no inhibition of other G protein subtypes. carboxylesterase 2 (CES2). YM-254890 inhibits platelet aggregation induced by

ADP by blocking the P2Y1 signal transduction

pathway, with an IC50 value below 0.6 μM. Purity: 98.55% Purity: >99.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 250 μg

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