Factor-Xa-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html Factor HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html XaFxaFactor Xa, a trypsin-like serine protease, is situated at the critical juncture between the intrinsic and extrinsic pathways, ca

2、talyzingthe conversion of prothrombin to thrombin, and hence plays a pivotal role in the final common pathway of the cascade and hasbecome an important target in the discovery and development of new anticoagulants. Factor Xa is a key protease of thecoagulation pathway whose activity is known to be i

3、n part modulated by binding to factor Va and sodium ions.Blood coagulation involves a complex cascade of enzymatic reactions, ultimately generating fibrin, the basis of all blood clots. Thiscascade is comprised of two arms, the intrinsic and extrinsic pathways which converge at factor Xa to form the

4、 common pathway.Factor Xa activates prothrombin to thrombin, which in turn catalyzes the conversion of fibrinogen to fibrin.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html Factor HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html HYPERLINK https:/www.MedChemE/Targets/Factor Xa.

5、html Xa HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html HYPERLINK https:/www.MedChemE/Targets/Factor Xa.html Inhibitors HYPERLINK https:/www.MedChemE/5-r-rivaroxaban.html 5-R-RivaroxabanCat. No.: HY-76948 HYPERLINK https:/www.MedChemE/Apixaban.html Apixaban(BMS-562247-01) Cat. No.: HY-506675-R-

6、Rivaroxaban is (R)-enantiomer of Rivaroxaban.Rivaroxaban (BAY 59-7939) is a highly potent andselective, direct Factor Xa (FXa) inhibitor,achieving a strong gain in anti-FXa potency (IC500.7 nM; K 0.4 nM).iApixaban (BMS-562247-01) is a highly selective,reversible and orally active inhibitor of Factor

7、Xa with K of 0.08 nM and 0.17 nM in human andirabbit, respectively. Apixaban is in developmentfor the prevention and treatment of variousthromboembolic diseases.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.99%Clinical Data: Launche

8、dSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/apixaban-13cd3.html Apixaban HYPERLINK https:/www.MedChemE/apixaban-13cd3.html HYPERLINK https:/www.MedChemE/apixaban-13cd3.html 13C,d3(BMS-562247-01 13C,d3) Cat. No.: HY-50667S HYPERLINK https:/www.MedChemE/asundexi

9、an.html Asundexian(BAY-2433334) Cat. No.: HY-137431Apixaban 13CD3 (BMS-562247-01 13CD3) is adeuterium labeled Apixaban. Apixaban is a highlyselective, reversible inhibitor of Factor Xawith K of 0.08 nM and 0.17 nM in human andirabbit, respectively.Purity: 99.47%Clinical Data: No Development Reported

10、Size: 1 mg, 5 mg, 10 mgAsundexian (BAY 2433334) is an orally activecoagulation factor Xia (FXIa) inhibitor. Asundexianbinds directly, potently, and reversibly to theactive site of FXIa and thereby inhibits itsactivity. Asundexian inhibits human FXIa in bufferwith an IC of 1 nM.50Purity: 98%Clinical

11、Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Betrixaban.html Betrixaban(PRT054021) Cat. No.: HY-10268 HYPERLINK https:/www.MedChemE/betrixaban-d6.html Betrixaban-d6Cat. No.: HY-10268SBetrixaban (PRT054021) is a highly potent,selective, and orally efficacious factor Xa(

12、fXa) inhibitor with IC of 1.5 nM.50Betrixaban D6 is a deuterium labeled Betrixaban.Betrixaban is a highly potent, selective, andorally efficacious factor Xa (fXa) inhibitor.Purity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.81%Clinical Data: No Development Rep

13、ortedSize: 1 mg HYPERLINK https:/www.MedChemE/bms-262084.html BMS-262084 HYPERLINK https:/www.MedChemE/bms-262084.html HYPERLINK https:/www.MedChemE/BMS-654457.html BMS-654457Cat. No.: HY-118969 Cat. No.: HY-12631BMS-262084 is a potent, selective and irreversibleinhibitor of factor XIa, with an IC o

14、f 2.8 nM50against human factor XIa. BMS-262084 also inhibitshuman tryptase (IC =5 nM). BMS-262084 exhibits50antithrombotic effects.BMS-654457 is a small-molecule, reversibleinhibitor of factor XIa (FXIa), binding with humanand rabbit FXIa with Ks of 0.2 and 0.42 nM,irespectively.Purity: 98%Clinical

15、Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bms-962212.html BMS-962212 HYPERLINK https:/www.MedChemE/bms-962212.html HYPERLINK https:/www.MedChemE/darexaban.html DarexabanCat. No.: HY-117290(YM150) Cat.

16、No.: HY-14853BMS-962212 is a direct, reversible, selectivefactor XIa (FXIa) inhibitor . BMS-962212 is welltolerated, with fast onset of pharmacodynamic (PD)responses and rapid elimination.Darexaban (YM150) is a potent, selective andorally active factor Xa (FXa) inhibitor with anIC of 54.6 nM. Darexa

17、ban shows high selectivity50against other related serine proteases, such astrypsin, thrombin, and kallikrein. Darexaban hasanticoagulant and antithrombotic effects.Purity: 98%Clinical Data: Phase 1Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.60%Clinical Data: No Development ReportedSize: 5 mg,

18、10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/delparantag.html Delparantag(PMX-60056) Cat. No.: HY-105240 HYPERLINK https:/www.MedChemE/edoxaban.html Edoxaban(DU-176) Cat. No.: HY-10264Delparantag (PMX-60056) is a salicylamidederi

19、vative and an effective unfractionated heparin(UFH) and low molecular weight heparin (LMWH)reversing agent. Delparantag shows ability toneutralize the anticoagulation and bleedingeffects of UFH and LMWH.Edoxaban (DU-176) is a selective, potent andorally active factor Xa (FXa) inhibitor with Ksiof 0.

20、561 nM and 2.98 nM for free FXa andprothrombinase, respectively. Edoxaban is ananticoagulant agent and can be used for strokeprevention.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.59%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/

21、www.MedChemE/edoxaban-impurity-4.html Edoxaban HYPERLINK https:/www.MedChemE/edoxaban-impurity-4.html HYPERLINK https:/www.MedChemE/edoxaban-impurity-4.html impurity HYPERLINK https:/www.MedChemE/edoxaban-impurity-4.html HYPERLINK https:/www.MedChemE/edoxaban-impurity-4.html 4Cat. No.: HY-134686 HYP

22、ERLINK https:/www.MedChemE/edoxaban-tosylate.html Edoxaban HYPERLINK https:/www.MedChemE/edoxaban-tosylate.html HYPERLINK https:/www.MedChemE/edoxaban-tosylate.html tosylate(DU-176b) Cat. No.: HY-10264AEdoxaban impurity 4 is an impurity of Edoxaban.Edoxaban (DU-176) is a selective, potent andorally

23、active factor Xa (FXa) inhibitor with Ksiof 0.561 nM and 2.98 nM for free FXa andprothrombinase, respectively.Edoxaban tosylate (DU-176b) is a selective, potentand orally active factor Xa (FXa) inhibitor withKis of 0.561 nM and 2.98 nM for free FXa andprothrombinase, respectively. Edoxaban tosylatei

24、s an anticoagulant agent and can be used forstroke prevention.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.47%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Edoxaban-tosylate-monohydrate.html Edoxaban HYPERLINK https:

25、/www.MedChemE/Edoxaban-tosylate-monohydrate.html HYPERLINK https:/www.MedChemE/Edoxaban-tosylate-monohydrate.html tosylate HYPERLINK https:/www.MedChemE/Edoxaban-tosylate-monohydrate.html HYPERLINK https:/www.MedChemE/Edoxaban-tosylate-monohydrate.html monohydrate(DU-176b monohydrate) Cat. No.: HY-1

26、0264B HYPERLINK https:/www.MedChemE/edoxaban-d6.html Edoxaban-d6(DU-176-d6) Cat. No.: HY-10264SEdoxaban tosylate monohydrate (DU-176bmonohydrate) is a selective, potent and orallyactive factor Xa (FXa) inhibitor with Ks ofi0.561 nM and 2.98 nM for free FXa andprothrombinase, respectively.Edoxaban-d6

27、 is deuterium labeled Edoxaban.Edoxaban (DU-176) is a selective, potent andorally active factor Xa (FXa) inhibitor with Kisof 0.561 nM and 2.98 nM for free FXa andprothrombinase, respectively.Purity: 99.95%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: N

28、o Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fitusiran.html Fitusiran HYPERLINK https:/www.MedChemE/fitusiran.html HYPERLINK https:/www.MedChemE/Fondaparinux-sodium.html Fondaparinux HYPERLINK https:/www.MedChemE/Fondaparinux-sodium.html HYPERLINK https:/www.MedChemE/Fondapar

29、inux-sodium.html sodium(ALN-AT3SC; SAR439774) Cat. No.: HY-132587 (Fondaparin sodium; SR-90107A) Cat. No.: HY-B0597Fitusiran (ALN-AT3SC), an small interfering RNA,specifically targets antithrombin (AT)messenger RNA to lower production of AT in theliver. Fitusiran increases thrombin generation andhas

30、 the potential for the research of thehemophilia.Fondaparinux sodium is an antithrombin-dependentfactor Xa inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/fxia-in-

31、1.html FXIa-IN-1 HYPERLINK https:/www.MedChemE/fxia-in-1.html HYPERLINK https:/www.MedChemE/fxia-in-6.html FXIa-IN-6Cat. No.: HY-128889 Cat. No.: HY-145349FXIa-IN-1 (compound EP-7041) is a potent -lactamcovalent heparin-derived factor XIa (fXIa)inhibitor.FXIa-IN-6 is a potent FXIa inhibitor withsele

32、ctivity against most of the relevant serineproteases (K = 0.3 nM).iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/fxia-in-7.html FXIa-IN-7 HYPERLINK https:/www.MedChemE/fxi

33、a-in-7.html HYPERLINK https:/www.MedChemE/fxia-in-8.html FXIa-IN-8Cat. No.: HY-145354 Cat. No.: HY-144658FXIa-IN-7 is a selective and orally bioavailablefactor XIa inhibitor with an IC value of 0.4 nM.50FXIa-IN-8 is a potent and selective FXIa inhibitorwith an IC of 14.2 nM. FXIa-IN-8 shows50antithr

34、ombotic activity without increasing thebleeding risk and obvious toxicitysup.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/Gabexate-mesylate.html Gabexate HYPERLINK https:/www.MedChemE/

35、Gabexate-mesylate.html HYPERLINK https:/www.MedChemE/Gabexate-mesylate.html mesylate(FOY) Cat. No.: HY-B0385 HYPERLINK https:/www.MedChemE/Heparin-sodium-salt.html Heparin HYPERLINK https:/www.MedChemE/Heparin-sodium-salt.html HYPERLINK https:/www.MedChemE/Heparin-sodium-salt.html sodium HYPERLINK h

36、ttps:/www.MedChemE/Heparin-sodium-salt.html HYPERLINK https:/www.MedChemE/Heparin-sodium-salt.html salt(Sodium heparin; Sodium heparinate) Cat. No.: HY-17567AGabexate mesylate is a Factor X inhibitor; serineprotease inhibitor .Heparin sodium salt (Sodium heparin) is ananticoagulant which binds rever

37、sibly toantithrombin III (ATIII) and greatly acceleratesthe rate at which ATIII inactivates coagulationenzymes thrombin factor IIa and factor Xa.Purity: 98.12%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 100 mgPurity: 98%Clinical Data: LaunchedSize: 100 mg, 500 mg, 1 g HYPERLINK https:/www.MedChe

38、mE/heparin-sodium-salt-mw-15kda.html Heparin HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html sodium HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15k

39、da.html salt HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html (MW HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html 15kDa)(Sodium heparin (MW 1

40、5kDa); Sodium heparinate (MW 15kDaC)at. No.: HY-17567C HYPERLINK https:/www.MedChemE/milvexian.html Milvexian(BMS-986177; JNJ-70033093) Cat. No.: HY-125856Heparin sodium salt (MW 15kDa) (Sodium heparin (MW15kDa) is a polymer of Heparin with the molecularweight of 15kDa.Milvexian (BMS-986177), an eff

41、ectiveantithrombotic agent, is an orally-bioavailable,reversible and direct inhibitor of human andrabbit factor XIa (FXIa) with K of 0.11, and 0.38inM, respectively.Purity: 98%Clinical Data: LaunchedSize: 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg,

42、50 mg HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-sodium.html O-Desmethyl HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-sodium.html HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-sodium.html apixaban HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-s

43、odium.html HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-sodium.html sulfate HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-sodium.html HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-sodium.html sodium HYPERLINK https:/www.MedChemE/o-desmethyl-apixaban-sulfate-so

44、dium.html HYPERLINK https:/www.MedChemE/Otamixaban.html OtamixabanCat. No.: HY-100652A(FXV673) Cat. No.: HY-70035O-Desmethyl apixaban sulfate sodium is a majorcirculating metabolite of Apixaban in humans.O-Desmethyl apixaban sulfate sodium inhibitsfactor X (FXa) with a K of 58 M.iOtamixaban(FXV673)

45、is a potent (Ki = 0.5 nM),selective, rapid acting, competitive andreversible fXa inhibitor that effectively inhibitsboth free and prothrombinase-bound fXa.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.97%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/razaxaban-hydrochloride.html Razaxaban HYPERLINK https:/www.MedChemE/razaxaban-hydrochloride.html HYPERLINK https:/www.MedChemE/razaxaban-hydrochloride.html hydrochloride HYPERLIN