P2Y-Receptor-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html P2Y HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html ReceptorP2Y receptors are a class of G protein-coupled receptors (GPCRs) activated by extracellular nucleotides (ATP, UTP, and

2、UDP). There are eight mammalian P2Y receptor subtypes (P2Y , P2Y , P2Y , P2Y , P2Y , P2Y , P2Y , and P2Y ). The P2Y receptors are expressed1 2 4 6 11 12 13 14in various cell types and play important roles in physiology and pathophysiology including inflammatory responses andneuropathic pain.The P2Y

3、family can be further divided into a subfamily of five P2Y , P2Y , P2Y , P2Y , and P2Y Rs (“P2Y -like”) that stimulate1 2 4 6 11 1phospholipase C (PLC) through G protein and a second subfamily of P2Y , P2Y , and P2Y Rs (“P2Y -like”) that inhibit adenylateq 12 13 14 12cyclase through G protein. Other

4、 effector pathways have been documented, such as coupling of the P2Y R to G as well as to G ini 11 s qsome cells to induce stimulation of cyclic AMP production.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html P2Y HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPERLINK

5、 https:/www.MedChemE/Targets/P2Y Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html Agonists

6、, HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html Antagonists HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html & HYPERLINK https:/www.MedChemE/Targets/P2Y Receptor.html HYPE

7、RLINK https:/www.MedChemE/Targets/P2Y Receptor.html Modulators HYPERLINK https:/www.MedChemE/2-methylthio-amp.html 2-Methylthio-AMP HYPERLINK https:/www.MedChemE/2-methylthio-amp.html (2-MeSAMP; 2-Methylthioadenosine5-monophosphate; 2-Methylthioadenosine 5-phosphate) Cat. No.: HY-125989 HYPERLINK ht

8、tps:/www.MedChemE/2-methylthio-amp-ditea.html 2-Methylthio-AMP HYPERLINK https:/www.MedChemE/2-methylthio-amp-ditea.html HYPERLINK https:/www.MedChemE/2-methylthio-amp-ditea.html diTEA HYPERLINK https:/www.MedChemE/2-methylthio-amp-ditea.html (2-MeSAMP diTEA; 2-Methylthioadenosine5-monophosphate diT

9、EA; ) Cat. No.: HY-125989B2-Methylthio-AMP (2-MeSAMP) is a selective anddirect P2Y antagonist. 2-Methylthio-AMP is an12inhibitor of ADP-dependent platelet aggregation.2-Methylthio-AMP (2-MeSAMP) diTEA is a selectiveand direct P2Y antagonist. 2-Methylthio-AMP12diTEA is an inhibitor of ADP-dependent p

10、lateletaggregation.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/2-methylthioadenosine-diphosphate-trisodium.html 2-Methylthioadenosine HYPERLINK https:/www.Med

11、ChemE/2-methylthioadenosine-diphosphate-trisodium.html HYPERLINK https:/www.MedChemE/2-methylthioadenosine-diphosphate-trisodium.html diphosphate HYPERLINK https:/www.MedChemE/2-methylthioadenosine-diphosphate-trisodium.html HYPERLINK https:/www.MedChemE/2-methylthioadenosine-diphosphate-trisodium.h

12、tml trisodium(2-Methylthio-ADP trisodium) Cat. No.: HY-108648 HYPERLINK https:/www.MedChemE/adenosine-2-5-diphosphate-sodium.html Adenosine HYPERLINK https:/www.MedChemE/adenosine-2-5-diphosphate-sodium.html HYPERLINK https:/www.MedChemE/adenosine-2-5-diphosphate-sodium.html 2,5-diphosphate HYPERLIN

13、K https:/www.MedChemE/adenosine-2-5-diphosphate-sodium.html HYPERLINK https:/www.MedChemE/adenosine-2-5-diphosphate-sodium.html sodiumCat. No.: HY-N77402-Methylthioadenosine diphosphate trisodium is apotent purinergic P2Y receptors agonist, withEC s of 19, 6.2, and 5 nM for human P2Y13,50mouse P2Y13

14、 and human P2Y12, respectively.Adenosine 2,5-diphosphate sodium is acompetitive P2Y1 antagonist. Adenosine2,5-diphosphate sodium exhibits non-selectiveantagonism at recombinant and human platelet P2X1receptors.Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No De

15、velopment ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/AZD1283.html AZD1283Cat. No.: HY-15799 HYPERLINK https:/www.MedChemE/BPTU.html BPTU(BMS-646786) Cat. No.: HY-13831AZD1283 is a potent antagonist of the P2Y12receptor with EC50 of 3.0 ug/kg/min, TI 10;with binding IC50 of 11 nM.

16、BPTU (BMS-646786) is a non-nucleotide P2Y1receptor allosteric antagonist with antithromboticactivity. BPTU is able to block the P2Y1 receptorlocated at the neuromuscular junction of thegastrointestinal tract.Purity: 99.11%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 10

17、0 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cangrelor-tetrasodium.html Cangrelor HYPERLINK https:/www.MedChemE/cangrelor-tetrasodium.html HYPERLINK https:/www.MedChemE/cangrelor-tetrasodium.html tetrasodium

18、 HYPERLINK https:/www.MedChemE/cangrelor-tetrasodium.html HYPERLINK https:/www.MedChemE/clopidogrel.html ClopidogrelCat. No.: HY-19638A Cat. No.: HY-15283Cangrelor tetrasodium, an adenosine triphosphateanalogue, is a reversible and selective plateletP2Y12 antagonist, with prompt and potentantiplatel

19、et effects.Clopidogrel is an orally active platelet inhibitorthat targets P2Y12 receptor. Clopidogrel is usedto inhibit blood clots in coronary artery disease,peripheral vascular disease, and cerebrovasculardisease.Purity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.5

20、7%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/Clopidogrel-hydrogen-sulfate.html Clopidogrel HYPERLINK https:/www.MedChemE/Clopidogrel-hydrogen-sulfate.html HYPERLINK https:/www.MedChemE/Clopidogrel-hydrogen-sulfate.html hydrogen HYPERLINK https:/www.MedChemE/Clopido

21、grel-hydrogen-sulfate.html HYPERLINK https:/www.MedChemE/Clopidogrel-hydrogen-sulfate.html sulfate HYPERLINK https:/www.MedChemE/Clopidogrel-hydrogen-sulfate.html (S)-(+)-Clopidogrel bisulfate; HYPERLINK https:/www.MedChemE/Clopidogrel-thiolactone.html Clopidogrel HYPERLINK https:/www.MedChemE/Clopi

22、dogrel-thiolactone.html HYPERLINK https:/www.MedChemE/Clopidogrel-thiolactone.html thiolactone(S)-(+)-Clopidogrel hydrogen sulfate) Cat. No.: HY-17459Cat. No.: HY-15876Clopidogrel hydrogen sulfate is an antiplateletagent to prevent blood clots. Clopidogrel hydrogensulfate inhibits CYP2B6 and CYP2C19

23、 with IC s50of 18.2 nM and 524 nM, respectively.Clopidogrel thiolactone is a P2Y12 receptorinhibitor, is a potent antiplatelet agent. Target:P2Y12 Clopidogrel thiolactone is the metabolicintermediate resulting from the first oxidativeactivation of clopidogrel.Purity: 99.75%Clinical Data: LaunchedSiz

24、e: 10 mM 1 mL, 100 mg, 500 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Diquafosol_tetrasodium_.html Diquafosol HYPERLINK https:/www.MedChemE/Diquafosol_tetrasodium_.h

25、tml HYPERLINK https:/www.MedChemE/Diquafosol_tetrasodium_.html tetrasodium(INS365) Cat. No.: HY-B0606 HYPERLINK https:/www.MedChemE/elinogrel.html Elinogrel(PRT060128) Cat. No.: HY-11021Diquafosol tetrasodium is a P2Y2 receptor agonistthat stimulates fluid and mucin secretion on theocular surface, a

26、s a topical treatment of dry eyedisease.Elinogrel (PRT060128) is a potent, direct acting,competitive, and reversible platelet P2Y12antagonist (IC =20 nM). It is orally and50intravenously available and has potentantiplatelet effects.Purity: 98.49%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg,

27、50 mg, 100 mgPurity: 98.68%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/MRS-2578.html MRS HYPERLINK https:/www.MedChemE/MRS-2578.html HYPERLINK https:/www.MedChemE/MRS-2578.html 2578 HYPERLINK https:/www.MedChemE/MRS-2578.html HYPERLINK https:/www.MedChemE/mr

28、s2179-tetrasodium.html MRS2179 HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium.html HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium.html tetrasodiumCat. No.: HY-13104 Cat. No.: HY-101308MRS 2578 is a selective and potent P2Y6 receptorantagonist with IC s of 37 nM (human) and 98 nM50(rat). MRS 25

29、78 exhibits insignificant activity atP2Y1, P2Y2, P2Y4, and P2Y11 receptors.MRS2179 tetrasodium is a competitive P2Y1receptor antagonist, with a K of 102 nM and abpA of 6.99 for turkey P2Y1 receptor. MRS21792tetrasodium is selective for P2Y1 over P2X1(IC =1.15 M), P2X3 (12.9 M), P2X2, P2X4, P2Y2,50P2

30、Y4, and P2Y6 receptors.Purity: 98.15%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium-hydrate.html MRS2179 HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium-hydrate.

31、html HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium-hydrate.html tetrasodium HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium-hydrate.html HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium-hydrate.html hydrate HYPERLINK https:/www.MedChemE/mrs2179-tetrasodium-hydrate.html HYPERLINK https:/www.Me

32、dChemE/mrs2279.html MRS2279Cat. No.: HY-101308A Cat. No.: HY-108657MRS2179 tetrasodium hydrate is a competitive P2Y1receptor antagonist, with a K of 102 nM and abpA of 6.99 for turkey P2Y1 receptor. MRS21792tetrasodium hydrate is selective for P2Y1 overP2X1 (IC =1.15 M), P2X3 (12.9 M), P2X2, P2X4,50

33、P2Y2, P2Y4, and P2Y6 receptors.MRS2279 is a selective and high affinity P2Y1receptor antagonist, with a K of 2.5 nM and aniIC of 51.6 nM. MRS2279 competitively inhibits50ADP-promoted platelet aggregation with an apparentaffnity (pK =8.05).BPurity: 99.0%Clinical Data: No Development ReportedSize: 5 m

34、gPurity: 98%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/mrs2365.html MRS2365 HYPERLINK https:/www.MedChemE/mrs2365.html HYPERLINK https:/www.MedChemE/mrs2395.html MRS2395Cat. No.: HY-108656 Cat. No.: HY-136501MRS2365 is a potent and selective P2Y1 receptoragonist w

35、ith an EC of 0.4 nM. MRS2365 shows50little agonist or antagonist activity at the P2Y12or P2Y13 receptors.MRS2395, an dipivaloyl derivative, is a potentP2Y12 receptor antagonist. MRS2395 inhibitsADP-induced platelet activation with a K of 3.6iM. MRS2395 inhibits cAMP induced by ADP in ratplatelets in

36、 the presence of PGE1 with an IC of 750M.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mrs2500-tetraammonium.html MRS2500 HYPERLINK https:/www.MedChemE/mrs2500-tetraammonium.html HYPERL

37、INK https:/www.MedChemE/mrs2500-tetraammonium.html tetraammonium HYPERLINK https:/www.MedChemE/mrs2500-tetraammonium.html HYPERLINK https:/www.MedChemE/mrs2768-tetrasodium-salt.html MRS2768 HYPERLINK https:/www.MedChemE/mrs2768-tetrasodium-salt.html HYPERLINK https:/www.MedChemE/mrs2768-tetrasodium-

38、salt.html tetrasodium HYPERLINK https:/www.MedChemE/mrs2768-tetrasodium-salt.html HYPERLINK https:/www.MedChemE/mrs2768-tetrasodium-salt.html saltCat. No.: HY-108658 Cat. No.: HY-108649AMRS2500 tetraammonium is a potent, selective andstable antagonist of the P2Y1 receptor (K=0.78inM for recombinant

39、human P2Y1 receptor). MRS2500tetraammonium inhibits the ADP-induced aggregationof human platelets with an IC value of 0.95 nM.50Antithrombotic activity.MRS2768 tetrasodium salt is a moderately potentand selective P2Y2 receptor agonist. MRS2768tetrasodium salt has a protective effect oncardiomyocytes

40、 from ischemic damage in vivo and invitro.Purity: 98%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/N6-_4-Hydroxybenzyl_adenosine.html N6-(4-Hydroxybenzyl)adenosine(Para-topoli

41、n riboside) Cat. No.: HY-18775 HYPERLINK https:/www.MedChemE/nf157.html NF157Cat. No.: HY-108672N6-(4-Hydroxybenzyl)adenosine is a inhibitor ofplatelet aggregation induced in vitro by collagenand their activity range was demonstrated (IC50:6.77-141 M).NF157 is a highly selective nanomolar P2Y11antag

42、onist with a pKi of 7.35. The IC50s are 463nM, 1811 M, 170 M for P2Y11 (K =44.3 nM), P2Y1i(K=187 M), P2Y2 (K=28.9 M), respectively.i iPurity: 99.29%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK

43、https:/www.MedChemE/nf340.html NF340 HYPERLINK https:/www.MedChemE/nf340.html HYPERLINK https:/www.MedChemE/nf546.html NF546Cat. No.: HY-108659 Cat. No.: HY-108661NF340 is a potent and selective P2Y11 receptorantagonist. NF340 inhibits the activity of P2Y11Rby completely combining with ATP-binding a

44、minoacid residues. NF340 ameliorates inflammation inhuman fibroblast-like synoviocytes and can be usedfor rheumatoid arthritis research.NF546 is a selective non-nucleotide P2Y11 agonistwith a pEC of 6.27. NF546 stimulates release50of interleukin-8 from human monocyte-deriveddendritic cells.Purity: 9

45、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Oral_antiplatelet_agent_1.html Oral HYPERLINK https:/www.MedChemE/Oral_antiplatelet_agent_1.html HYPERLINK https:/www.MedChemE/Oral_antiplatelet_age

46、nt_1.html antiplatelet HYPERLINK https:/www.MedChemE/Oral_antiplatelet_agent_1.html HYPERLINK https:/www.MedChemE/Oral_antiplatelet_agent_1.html agent HYPERLINK https:/www.MedChemE/Oral_antiplatelet_agent_1.html HYPERLINK https:/www.MedChemE/Oral_antiplatelet_agent_1.html 1 HYPERLINK https:/www.MedC

47、hemE/Oral_antiplatelet_agent_1.html HYPERLINK https:/www.MedChemE/p2y2r-gpr17-antagonist-1.html P2Y2R/GPR17 HYPERLINK https:/www.MedChemE/p2y2r-gpr17-antagonist-1.html HYPERLINK https:/www.MedChemE/p2y2r-gpr17-antagonist-1.html antagonist HYPERLINK https:/www.MedChemE/p2y2r-gpr17-antagonist-1.html H

48、YPERLINK https:/www.MedChemE/p2y2r-gpr17-antagonist-1.html 1Cat. No.: HY-111755 Cat. No.: HY-146486Oral antiplatelet agent 1 is a potent antiplateletagent with an IC50 of 2.94 M in vitro as well asantithrombotic efficacy in a rat model. P2Yreceptor antagonist.P2Y2R/GPR17 antagonist 1 (Compound 14m)

49、is a dualP2Y R2 and GPR17 antagonist with IC50 values of3.17 M and 1.67 M against P2Y R and GPR17,2respectively. P2Y2R/GPR17 antagonist 1 showsexcellent metabolic stability in human livermicrosomes.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Developm

50、ent ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pptn.html PPTN HYPERLINK https:/www.MedChemE/pptn.html HYPERLINK https:/www.MedChemE/pptn-hydrochloride.html PPTN HYPERLINK https:/www.MedChemE/pptn-hydrochloride.html HYPERLINK https:/www.MedChemE/pptn-hydrochloride.html hydrochlorideCat. N

51、o.: HY-110322A Cat. No.: HY-110322PPTN is a potent, high-affinity, competitive andhighly selective P2Y14 receptor antagonist witha K value of 434 pM. PPTN exhibits no agonistBor antagonist effect at the P2Y1, P2Y2, P2Y4,P2Y6, P2Y11, P2Y12, or P2Y13 receptors.Anti-inflammatory and immune activity.PPT

52、N hydrochloride is a potent, high-affinity,competitive and highly selective P2Y14 receptorantagonist with a K value of 434 pM. PPTNBhydrochloride exhibits no agonist or antagonisteffect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11,P2Y12, or P2Y13 receptors.Purity: 98%Clinical Data: No Development ReportedSi

53、ze: 1 mgPurity: 99.89%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/prasugrel.html Prasugrel HYPERLINK https:/www.MedChemE/prasugrel.html HYPERLINK https:/www.MedChemE/Prasugrel-Maleic-acid.html Prasugrel HYPERLINK https:/www.MedChemE/Pra

54、sugrel-Maleic-acid.html HYPERLINK https:/www.MedChemE/Prasugrel-Maleic-acid.html (Maleic HYPERLINK https:/www.MedChemE/Prasugrel-Maleic-acid.html HYPERLINK https:/www.MedChemE/Prasugrel-Maleic-acid.html acid)(PCR 4099) Cat. No.: HY-15284 (PCR 4099 (Maleic acid) Cat. No.: HY-15284BPrasugrel (PCR 4099

55、), a thienopyridine andprodrug, inhibits platelet function. Prasugrel isan orally active and potent P2Y12 receptorantagonist, and inhibits ADP-induced plateletaggregation.Prasugrel (PCR 4099) Maleic acid is athienopyridine and prodrug, inhibits plateletfunction. Prasugrel Maleic acid is an orallyact

56、ive and potent P2Y12 receptor antagonist, andinhibits ADP-induced platelet aggregation.Purity: 99.85%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/prasu

57、grel-hydrochloride.html Prasugrel HYPERLINK https:/www.MedChemE/prasugrel-hydrochloride.html HYPERLINK https:/www.MedChemE/prasugrel-hydrochloride.html hydrochloride(PCR 4099 hydrochloride) Cat. No.: HY-15284A HYPERLINK https:/www.MedChemE/prasugrel-d3.html Prasugrel-d3(PCR 4099-d3) Cat. No.: HY-152

58、84S1Prasugrel hydrochloride (PCR 4099 hydrochloride),a thienopyridine and prodrug, inhibits plateletfunction. Prasugrel hydrochloride is an orallyactive and potent P2Y12 receptor antagonist, andinhibits ADP-induced platelet aggregation.Prasugrel-d3 (PCR 4099-d3) is the deuteriumlabeled Prasugrel. Pr

59、asugrel (PCR 4099), athienopyridine and prodrug, inhibits plateletfunction. Prasugrel is an orally active and potentP2Y12 receptor antagonist, and inhibitsADP-induced platelet aggregation.Purity: 99.57%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 98%Clinical Data: No Development Re

60、portedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/prasugrel-d5.html Prasugrel-d5(PCR 4099-d5) Cat. No.: HY-15284S HYPERLINK https:/www.MedChemE/psb-0474.html PSB HYPERLINK https:/www.MedChemE/psb-0474.html HYPERLINK https:/www.MedChemE/psb-0474.html 0474Cat. No.: HY-108654Prasugrel-d5 is deuteriu