Thrombin-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Thrombin.html ThrombinThrombin is a Na+-activated, serine protease which is activated by the enzymatic cleavage of two sites on prothrombin by activatedFactor X. Thrombin exists in two allosteric forms, slow (S) and fast (F), target toward anticoagulant and pro

2、coagulant activities.Thrombin is the main effector protease in primary hemostasis by activating platelets and plays a key role in secondary hemostasis.Besides its well-known functions in hemostasis, thrombin also plays a role in various non-hemostatic biological andpathophysiologic processes, predom

3、inantly mediated through activation of protease-activated receptors (PARs). PAR-1, PAR-3, andPAR-4 are cleaved by thrombin, whereas PAR-2 is cleaved by trypsin. Thrombin also plays a crucial role in the migration andmetastasis of human cancer cells.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Target

4、s/Thrombin.html Thrombin HYPERLINK https:/www.MedChemE/Targets/Thrombin.html HYPERLINK https:/www.MedChemE/Targets/Thrombin.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Thrombin.html HYPERLINK https:/www.MedChemE/Targets/Thrombin.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Thrombi

5、n.html HYPERLINK https:/www.MedChemE/Targets/Thrombin.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Thrombin.html HYPERLINK https:/www.MedChemE/Targets/Thrombin.html & HYPERLINK https:/www.MedChemE/Targets/Thrombin.html HYPERLINK https:/www.MedChemE/Targets/Thrombin.html Activators HYPERLIN

6、K https:/www.MedChemE/AEBSF.html AEBSF HYPERLINK https:/www.MedChemE/AEBSF.html HYPERLINK https:/www.MedChemE/AEBSF.html hydrochlorideCat. No.: HY-12821 HYPERLINK https:/www.MedChemE/argatroban.html Argatroban(MD-805; MCI-9038; Argipidine) Cat. No.: HY-B0375AEBSF hydrochloride is an irreversible inh

7、ibitorof serine proteases, such as chymotrypsin,kallikrein, plasmin, thrombin, and trypsin.Argatroban (MD-805) is a direct, selectivethrombin inhibitor.Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg, 200 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK htt

8、ps:/www.MedChemE/Argatroban-monohydrate.html Argatroban HYPERLINK https:/www.MedChemE/Argatroban-monohydrate.html HYPERLINK https:/www.MedChemE/Argatroban-monohydrate.html monohydrate HYPERLINK https:/www.MedChemE/Argatroban-monohydrate.html (MD-805 monohydrate; MCI-9038monohydrate; Argipidine monoh

9、ydrate) Cat. No.: HY-B0375A HYPERLINK https:/www.MedChemE/argatroban-d3.html Argatroban-d3Cat. No.: HY-B0375SArgatroban (monohydrate) (MD-805 (monohydrate) isa direct, selective thrombin inhibitor.Argatroban-d3 is the deuterium labeled Argatroban.Argatroban (MD-805) is a direct, selectivethrombin in

10、hibitor.Purity: 99.96%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/atecegatran-metoxil.html Atecegatran HYPERLINK https:/www.MedChemE/atecegatran-metoxil.html HYPERLINK https:/www.MedChem

11、E/atecegatran-metoxil.html metoxil(AZD0837; Atecegatran fexenetil) Cat. No.: HY-10273 HYPERLINK https:/www.MedChemE/bay-1217224.html BAY HYPERLINK https:/www.MedChemE/bay-1217224.html HYPERLINK https:/www.MedChemE/bay-1217224.html 1217224Cat. No.: HY-142661Atecegatran metoxil is a oral anticoagulant

12、, whichinhibits thrombin factor II and is used inthromboembolic disorders. In vivo, Atecegatranmetoxil is converted to AR-H067637, a selectiveand reversible direct thrombin inhibitor.BAY 1217224 is a neutral, non-prodrug Thrombininhibitor with good oral pharmacokinetics.Purity: 98%Clinical Data: No

13、Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bivalirudin.html Bivalirudin HYPERLINK https:/www.MedChemE/bivalirudin.html HYPERLINK https:/www.MedChemE/Bivalirudin-Trifluoroacetate.html Bivalirudin HYPERLINK https:

14、/www.MedChemE/Bivalirudin-Trifluoroacetate.html HYPERLINK https:/www.MedChemE/Bivalirudin-Trifluoroacetate.html TFACat. No.: HY-P1929 Cat. No.: HY-15664Bivalirudin, a peptide anticoagulant, is a directthrombin inhibitor for anticoagulation in thesetting of invasive cardiology, particularlypercutaneo

15、us coronary intervention.Bivalirudin TFA is a synthetic 20 residue peptidewhich reversibly inhibits thrombin.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.89%Clinical Data: LaunchedSize: 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Dabigatran.html Dabigatran HYPERLINK https:/www

16、.MedChemE/Dabigatran.html HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester.html Dabigatran HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester.html HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester.html (ethyl HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester.html HYPERLINK https:/www.Med

17、ChemE/dabigatran-ethyl-ester.html ester)(BIBR 953; BIBR 953ZW) Cat. No.: HY-10163Cat. No.: HY-17378Dabigatran (BIBR 953), an oral anticoagulant, is areversible, potent, competitive direct thrombininhibitor (K=4.5 nM). Dabigatran (BIBR 953) alsoiinhibits thrombin-induced platelet aggregation(IC =10 n

18、M).50Dabigatran ethyl ester is an emerging oralanticoagulant which is a direct inhibitor ofthrombin activity. IC50 value: Target: thrombinDabigatran provides a stable anticoagulationeffect without any need to perform periodicallaboratory controls.Purity: 98.65%Clinical Data: Phase 4Size: 5 mg, 10 mg

19、, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Dabigatran-etexilate.html Dabigatran HYPERLINK https:/www.MedChemE/Dabigatran-etexilate.html HYPERLINK htt

20、ps:/www.MedChemE/Dabigatran-etexilate.html etexilate(BIBR 1048) Cat. No.: HY-10274 HYPERLINK https:/www.MedChemE/Dabigatran-etexilate-mesylate.html Dabigatran HYPERLINK https:/www.MedChemE/Dabigatran-etexilate-mesylate.html HYPERLINK https:/www.MedChemE/Dabigatran-etexilate-mesylate.html etexilate H

21、YPERLINK https:/www.MedChemE/Dabigatran-etexilate-mesylate.html HYPERLINK https:/www.MedChemE/Dabigatran-etexilate-mesylate.html mesylate(BIBR 1048MS; Dabigatran etexilate methanesulfonate) Cat. No.: HY-10274ADabigatran etexilate (BIBR 1048) is an orallyactive prodrug of Dabigatran (a direct inhibit

22、orof thrombin). Dabigatran etexilate hasanticoagulant effects and is used for theprophylaxis of venousthromboembolism and strokedue to atrial fibrillation.Dabigatran etexilate mesylate (BIBR 1048MS) is anorally active prodrug of Dabigatran (a directinhibitor of thrombin). Dabigatran etexilatemesylat

23、e has anticoagulant effects and is used forthe prophylaxis of venousthromboembolism andstroke due to atrial fibrillation.Purity: 99.75%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.60%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HY

24、PERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.html Dabigatran HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.html HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.html ethyl HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.ht

25、ml HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.html ester HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.html HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Dabigatran-ethyl-ester-hydrochl

26、oride.html HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester-d3-hydrochloride.html Dabigatran HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester-d3-hydrochloride.html ethyl HYPERLINK https:/www.MedChemE/dabigatran-ethyl-

27、ester-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester-d3-hydrochloride.html ester-d3 HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/dabigatran-ethyl-ester-d3-hydrochloride.html hydrochlorideCat. No.: HY-77521 Cat. N

28、o.: HY-77521SDabigatran ethyl ester hydrochloride is a potentinhibitor of ribosyldihydronicotinamidedehydrogenase (NQO2) with an IC value of 0.8 M50and a thrombin inhibitor.Dabigatran ethyl ester-d3 hydrochloride is thedeuterium labeled Dabigatran (ethyl esterhydrochloride).Purity: 98%Clinical Data:

29、 LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dabigatran-13c-d3.html Dabigatran-13C,d3(BIBR 953-13C,d3; BIBR 953ZW-13C,d3) Cat. No.: HY-10163S3 HYPERLINK https:/www.MedChemE/dabigatran-d3.ht

30、ml Dabigatran-d3(BIBR 953-d3; BIBR 953ZW-d3) Cat. No.: HY-10163S1Dabigatran-13C,d3 is the 13C- and deuteriumlabeled. Dabigatran (BIBR 953), an oralanticoagulant, is a reversible, potent,competitive direct thrombin inhibitor (Ki=4.5 nM).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 m

31、gDabigatran-d3 (BIBR 953-d3) is the deuteriumlabeled Dabigatran. Dabigatran (BIBR 953), an oralanticoagulant, is a reversible, potent,competitive direct thrombin inhibitor (K=4.5inM). Dabigatran (BIBR 953) also inhibitsthrombin-induced platelet aggregation (IC =10 nM).50Purity: 98%Clinical Data: No

32、Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dabigatran-d4.html Dabigatran-d4 HYPERLINK https:/www.MedChemE/dabigatran-d4.html HYPERLINK https:/www.MedChemE/Dabigatran-D4-hydrochloride.html Dabigatran-d4 HYPERLINK https:/www.MedChemE/Dabigatran-D4-hydrochloride.html HYPERLINK h

33、ttps:/www.MedChemE/Dabigatran-D4-hydrochloride.html hydrochloride(BIBR 953-d4; BIBR 953ZW-d4) Cat. No.: HY-10163S (BIBR-953-d4 hydrochloride) Cat. No.: HY-10163ASDabigatran-d4 is deuterium labeled Dabigatran.Dabigatran (BIBR 953), an oral anticoagulant, is areversible, potent, competitive direct thr

34、ombininhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) alsoinhibits thrombin-induced platelet aggregation(IC50=10 nM).Dabigatran (BIBR-953) D4 hydrochloride isdeuterium labeled Dabigatran, which is areversible and selective, direct thrombininhibitor (DTI) with a K value of 4.5 nM.iPurity: 98%Clinical Dat

35、a: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/2-4,5-Bis_4-methoxyphenyl_-2-thiazolyl-1H-pyrrole-1-acetic_acid.html Desethyl HYPERLINK https:/www.MedChemE/2-4,5-Bis_4-methoxyphenyl_-2-thiazolyl-1H-pyrrole-1

36、-acetic_acid.html HYPERLINK https:/www.MedChemE/2-4,5-Bis_4-methoxyphenyl_-2-thiazolyl-1H-pyrrole-1-acetic_acid.html KBT-3022 HYPERLINK https:/www.MedChemE/2-4,5-Bis_4-methoxyphenyl_-2-thiazolyl-1H-pyrrole-1-acetic_acid.html HYPERLINK https:/www.MedChemE/edoxaban.html EdoxabanCat. No.: HY-U00039(DU-

37、176) Cat. No.: HY-10264Desethyl KBT-3022 is the main active metabolite ofthe new antiplatelet agent, KBT-3022.Edoxaban (DU-176) is a selective, potent andorally active factor Xa (FXa) inhibitor with Ksiof 0.561 nM and 2.98 nM for free FXa andprothrombinase, respectively. Edoxaban is ananticoagulant

38、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 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/edoxaban-impurity-4.html Edoxaban HYPERLINK https:/www.MedChemE/ed

39、oxaban-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 HYPERLINK https:/www.MedChemE/edoxaban-tosylate.html Edoxaban HYPERLINK https:/www

40、.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 active factor Xa (FXa) inhibitor with Ksiof 0.561 nM and 2.98 nM for free FXa a

41、ndprothrombinase, 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 tosylateis an anticoagulant agent and can be used forstroke prevention.Purity: 98%Clinic

42、al 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:/www.MedChemE/Edoxaban-tosylate-monohydrate.html HYPERLINK https:/www.MedChemE/

43、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-10264B HYPERLINK https:/www.MedChemE/edoxaban-d6.html Edoxaban-d6(DU-176-d6) Cat

44、. 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 is deuterium labeled Edoxaban.Edoxaban (DU-176) is a selective, potent andoral

45、ly 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: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Heparin.ht

46、ml Heparin HYPERLINK https:/www.MedChemE/Heparin.html HYPERLINK https:/www.MedChemE/Heparin_Lithium_salt.html Heparin HYPERLINK https:/www.MedChemE/Heparin_Lithium_salt.html HYPERLINK https:/www.MedChemE/Heparin_Lithium_salt.html Lithium HYPERLINK https:/www.MedChemE/Heparin_Lithium_salt.html HYPERL

47、INK https:/www.MedChemE/Heparin_Lithium_salt.html saltCat. No.: HY-17567 Cat. No.: HY-17567BHeparin is a highly sulfatedglycosaminoglycan,that is widely used as aninjectable anticoagulant, and has the highestnegative charge density of any known biologicalmolecule. Heparin significantly inhibitsexoso

48、me-cell interactions.Heparin Lithium salt is an anticoagulant whichbinds reversibly to antithrombin III (ATIII).Heparin Lithium salt significantly inhibitsexosome-cell interactions.Purity: 98%Clinical Data: LaunchedSize: 10 mg(10 mg mL in Water)Purity: 98%Clinical Data: LaunchedSize: 10 mg(10 mg mL

49、in Water), 100 mg, 500 mg 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 https:/www.MedChemE/Heparin-sodium-salt.html HYPERLINK https:/www.MedChemE/Heparin-s

50、odium-salt.html salt HYPERLINK https:/www.MedChemE/Heparin-sodium-salt.html HYPERLINK https:/www.MedChemE/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:/

51、www.MedChemE/heparin-sodium-salt-mw-15kda.html HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.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

52、-15kda.html HYPERLINK https:/www.MedChemE/heparin-sodium-salt-mw-15kda.html 15kDa)(Sodium heparin; Sodium heparinate) Cat. No.: HY-17567A (Sodium heparin (MW 15kDa); Sodium heparinate (MW 15kDaC)at. No.: HY-17567CHeparin sodium salt (Sodium heparin) is ananticoagulant which binds reversibly toantith

53、rombin III (ATIII) and greatly acceleratesthe rate at which ATIII inactivates coagulationenzymes thrombin factor IIa and factor Xa.Heparin sodium salt (MW 15kDa) (Sodium heparin (MW15kDa) is a polymer of Heparin with the molecularweight of 15kDa.Purity: 98%Clinical Data: LaunchedSize: 100 mg, 500 mg

54、, 1 gPurity: 98%Clinical Data: LaunchedSize: 100 mg, 500 mg HYPERLINK https:/www.MedChemE/idraparinux-sodium.html Idraparinux HYPERLINK https:/www.MedChemE/idraparinux-sodium.html HYPERLINK https:/www.MedChemE/idraparinux-sodium.html sodium HYPERLINK https:/www.MedChemE/idraparinux-sodium.html HYPER

55、LINK https:/www.MedChemE/Inogatran.html Inogatran(SANORG 34006; SR-34006) Cat. No.: HY-19691 (H-314-27) Cat. No.: HY-19660Idraparinux (sodium) is a polymethylated syntheticpentasaccharide known to interact with theantithrombin III and act as anticoagulant.Inogatran (H-314-27) is a synthetic thrombin

56、inhibitor, developed for the possible treatmentand prophylaxis of arterial and venous thromboticdiseases.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERL

57、INK https:/www.MedChemE/melagatran.html MelagatranCat. No.: HY-129056 HYPERLINK https:/www.MedChemE/metolazone.html Metolazone(SR-720-22) Cat. No.: HY-B0209Melagatran is a direct and orally active inhibitorof thrombin, without interacting with any otherenzymes in the coagulation cascade or fibrinoly

58、ticenzymes aside from thrombin.Metolazone (SR-720-22) is primarily used to treatcongestive heart failure and high blood pressure.Purity: 98%Clinical Data:Size: 1 mg, 5 mg, 10 mgPurity: 99.86%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/metolazone-d7.html Metol

59、azone-d7(SR-720-22-d7) Cat. No.: HY-B0209S HYPERLINK https:/www.MedChemE/Napsagatran_(hydrate).html Napsagatran HYPERLINK https:/www.MedChemE/Napsagatran_(hydrate).html HYPERLINK https:/www.MedChemE/Napsagatran_(hydrate).html hydrate(Ro 46-6240 hydrate; Ro 46-6240/010 hydrate) Cat. No.: HY-15759AMet

60、olazone-d7 is deuterium labeled Metolazone.Metolazone (SR-720-22) is primarily used to treatcongestive heart failure and high blood pressure.Napsagatran hydrate is a novel and specificthrombin inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Dev