P2Y

P2Y receptors are a class of G protein-coupled receptors (GPCRs) activated by extracellular (ATP, UTP, and UDP). There are eight mammalian subtypes (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, , P2Y13, and P2Y14). The P2Y receptors are expressed in various cell types and play important roles in physiology and pathophysiology including inflammatory responses and neuropathic pain.

The P2Y family can be further divided into a subfamily of five P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs (“P2Y1-like”) that stimulate phospholipase C (PLC) through Gq protein and a second subfamily of P2Y12, P2Y13, and P2Y14Rs (“P2Y12-like”) that inhibit adenylate cyclase through Gi protein. Other effector pathways have been documented, such as coupling of the P2Y11R to Gs as well as to Gq in some cells to induce stimulation of cyclic AMP production.

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

2-Methylthioadenosine diphosphate trisodium 2',5'-diphosphate (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- P2Y1 receptor with EC50 of 3.0 ug/kg/min, TI >10; receptor allosteric antagonist with 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 Cat. No.: HY-19638A Cat. No.: HY-15283

Cangrelor tetrasodium, an 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. Target: sticking together and prevents them from forming P2Y12 Clopidogrel thiolactone is the metabolic harmful clots. intermediate resulting from the first oxidative activation of clopidogrel.

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

Denufosol tetrasodium tetrasodium (INS37217) Cat. No.: HY-U00196 (INS365) Cat. No.: HY-B0606

Denufosol tetrasodium (INS37217) is a long-acting Diquafosol tetrasodium is a P2Y2 receptor agonist

P2Y2 receptor agonist, which exhibits an that stimulates fluid and mucin secretion on the

EC50 of ~10 μM for P2Y2 receptor activation. ocular surface, as a topical treatment of dry eye disease.

Purity: >98% Purity: 98.49% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Elinogrel MRS 2578 (PRT060128) Cat. No.: HY-11021 Cat. No.: HY-13104

Elinogrel (PRT060128) is a potent, direct acting, MRS 2578 is a selective and potent P2Y6 receptor competitive, and reversible platelet P2Y12 antagonist with IC50s of 37 nM (human) and 98 nM antagonist (IC50=20 nM). It is orally and (rat). MRS 2578 exhibits insignificant activity at intravenously available and has potent P2Y1, P2Y2, P2Y4, and P2Y11 receptors. antiplatelet effects.

Purity: ≥98.0% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

MRS2179 tetrasodium hydrate MRS2279 Cat. No.: HY-101308A Cat. No.: HY-108657

MRS2179 tetrasodium hydrate is a competitive P2Y1 MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Kb of 102 nM and a receptor antagonist, with a Ki of 2.5 nM and an pA of 6.99 for turkey P2Y1 receptor. MRS2179 2 IC50 of 51.6 nM. MRS2279 competitively inhibits tetrasodium hydrate is selective for P2Y1 over ADP-promoted platelet aggregation with an apparent P2X1 (IC =1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, 50 affnity (pKB=8.05). P2Y2, P2Y4, and P2Y6 receptors. Purity: ≥99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg

MRS2500 tetraammonium MRS2698 Cat. No.: HY-108658 Cat. No.: HY-111075

MRS2500 tetraammonium is a potent, selective and MRS2698 is a potent and highly selective P2Y2 stable antagonist of the P2Y1 receptor (Ki=0.78 receptor agonist with an EC50 of 8 nM. MRS2698 nM for recombinant human P2Y1 receptor). MRS2500 is >300-fold P2Y2-selective versus the P2Y4 and tetraammonium inhibits the ADP-induced aggregation P2Y6 receptors. of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 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: 99.29% 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

NF546 Oral antiplatelet agent 1 Cat. No.: HY-108661 Cat. No.: HY-111755

NF546 is a selective non-nucleotide P2Y11 agonist Oral antiplatelet agent 1 is a potent antiplatelet with a pEC50 of 6.27. NF546 stimulates release agent with an IC50 of 2.94 μM in vitro as well as of interleukin-8 from human monocyte-derived antithrombotic efficacy in a rat model. P2Y dendritic cells. receptor antagonist.

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

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PPTN PPTN hydrochloride Cat. No.: HY-110322A Cat. No.: HY-110322

PPTN is a potent, high-affinity, competitive and PPTN hydrochloride is a potent, high-affinity, highly selective P2Y14 receptor antagonist with competitive and highly selective P2Y14 receptor

a KB value of 434 pM. PPTN exhibits no agonist antagonist with a KB value of 434 pM. PPTN or antagonist effect at the P2Y1, P2Y2, P2Y4, hydrochloride exhibits no agonist or antagonist P2Y6, P2Y11, P2Y12, or P2Y13 receptors. effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, Anti-inflammatory and immune activity. P2Y12, or P2Y13 receptors. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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

Prasugrel (PCR 4099), a and Prasugrel (PCR 4099) Maleic acid is a , 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: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

Prasugrel hydrochloride PSB-1114 tetrasodium (PCR 4099 hydrochloride) Cat. No.: HY-15284A Cat. No.: HY-110092

Prasugrel hydrochloride (PCR 4099 hydrochloride), PSB-1114 tetrasodium is a potent, enzymatically

a thienopyridine and prodrug, inhibits platelet stable, and subtype-selective P2Y2 receptor

function. Prasugrel hydrochloride is an orally agonist with an EC50 of 134 nM. PSB-1114 active and potent P2Y12 receptor antagonist, and tetrasodium displays >50-fold selectivity

inhibits ADP-induced platelet aggregation. versus the P2Y4 (EC50 of 9.3 μM) and P2Y6

(EC50 of 7.0 μM) receptors. 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

TAK-024 Cat. No.: HY-100254 (AZD6140; AR-C 126532XX) Cat. No.: HY-10064

TAK-024 is a platelet inhibitor with IC50s of 31, Ticagrelor (AZD6140) is a reversible oral P2Y12 79 and 51 nM in human, monkey and guinea pig, receptor antagonist for the treatment of platelet respectively. aggregation.

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

trans-R-138727MP 5'-diphosphate sodium salt (Prasugrel metabolite R-138727MP) Cat. No.: HY-136588 Cat. No.: HY-W010820

trans-R-138727MP (Prasugrel metabolite R-138727MP) Uridine 5'-diphosphate sodium salt is a potent,

is the active metabolite derivative of selective P2Y6 receptor native agonist

Prasugrel (HY-15284). Prasugrel, a (EC50=300 nM; pEC50=6.52) and a potent P2Y14

thienopyridine and prodrug, inhibits platelet antagonist (pEC50=7.28). function.

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

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Uridine 5′-diphosphoglucose disodium salt glucose (UDP-D-Glucose disodium salt) Cat. No.: HY-N7032 Cat. No.: HY-113044

Uridine 5′-diphosphoglucose disodium salt Uridine diphosphate glucose is the precursor of (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine animal tissues and in some microorganisms. diphosphate glucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR1.. Purity: 99.52% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg

Uridine-5'-diphosphate disodium salt Vicagrel Cat. No.: HY-W010832 Cat. No.: HY-118284

Uridine-5'-diphosphate disodium salt is a potent, Vicagrel, an acetate derivative of Clopidogrel, is selective P2Y6 receptor native agonist a P2Y12 platelet inhibitor potentially for the

(EC50=300 nM; pEC50=6.52 for human P2Y6 treatment of thrombosis, the substrate of receptor). carboxylesterase 2 (CES2).

Purity: 98.01% Purity: 98.55% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

YM-254890 Cat. No.: HY-111557

YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by

ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM. Purity: ≥95.0% Clinical Data: No Development Reported Size: 250 μg

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