HCV-Protease-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html HCV HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html ProteaseHCV NS3-4A serine protease is a complex composed of NS3 and its cofactor NS4A. It harbours serine protease as well asNT

2、Pase/RNA helicase activities and is essential for viral polyprotein processing, RNA replication and virion formation.The HCV NS3/4A protease efficiently cleaves and inactivates two important signaling molecules in the sensory pathways that reactto HCV pathogen-associated molecular patterns (PAMPs) t

3、o induce interferons (IFNs), i.e., mitochondrial antiviral signaling protein(MAVS) and Toll-IL-1 receptor domain-containing adaptor inducing IFN- (TRIF). HCV infection is associated with chronic liverdisease, including hepatic steatosis, fibrosis, cirrhosis, and hepatocellular carcinoma. The NS3-4A

4、serine protease of HCV has beenone of the most attractive targets for developing specific antiviral agents against HCV.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html HCV HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html HYPERLINK https:/www.MedChemE/Targets/HCV Protease

5、.html Protease HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html & HYPERLINK https:/www.MedChemE/Targets/HCV Protea

6、se.html HYPERLINK https:/www.MedChemE/Targets/HCV Protease.html Antagonists HYPERLINK https:/www.MedChemE/ACH-806.html ACH-806(GS9132) Cat. No.: HY-19512 HYPERLINK https:/www.MedChemE/al-611.html AL-611Cat. No.: HY-145374ACH-806 is an NS4A antagonist which can inhibitHepatitis C Virus (HCV) replicat

7、ion with anEC of 14 nM.50AL-611 is an HCV NS5B polymerase inhibitor(EC = 5 nM).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Asunaprevir.html Asunaprevir(BMS-650032) Cat. No.: HY-1443

8、4 HYPERLINK https:/www.MedChemE/azd-7295.html AZD-7295Cat. No.: HY-111087Asunaprevir (BMS-650032) is a potent and orallybioavailable hepatitis C virus (HCV) NS3 proteaseinhibitor, with IC of 0.2 nM-3.5 nM. Asunaprevir50inhibits SARS-CoV-2 3CLpro activity.AZD-7295 is a HCV NS5A protein inhibitor, wit

9、han EC of 7 nM for GT-1b replicon.50Purity: 99.71%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bi-653048.html BI HYPERLINK https:/www.MedChemE/bi-653048.html HYPERLINK https:/www.MedCh

10、emE/bi-653048.html 653048 HYPERLINK https:/www.MedChemE/bi-653048.html HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html BI HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html 653048 HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html

11、 HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html phosphateCat. No.: HY-12946 Cat. No.: HY-12946ABI 653048 is a selective and orally activenonsteroidal glucocorticoid (GC) agonistwith an IC value of 55 nM. BI 653048 inhibits50CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4isoforms activity and reduc

12、es affinity for thehERG ion channel (IC 30 M).50Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mgBI 653048 phosphate is a selective and orallyactive nonsteroidal glucocorticoid(GC) agonist with an IC value of 55 nM.50Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bi-

13、1230.html BI-1230 HYPERLINK https:/www.MedChemE/bi-1230.html HYPERLINK https:/www.MedChemE/bms-986144.html BMS-986144Cat. No.: HY-126973 Cat. No.: HY-131905SBI-1230 is potent and digit nanomolar inhibitor ofHCV NS3 protease and of viral replication. BI-1230is also highly selective against otherserin

14、e/cysteine proteases. BI-1230 shows goodPharmacokinetic(PK) activity.BMS-986144 is a third-generation, pan-genotype(GT) NS3/4A protease inhibitor. BMS-986144inhibits HCV replicon with EC s of 2.3, 0.7,501.0, 12, 8.0, and 5.8 nM for GT-1a, GT-1b, GT-2a,GT-3a, 1a R155X, and 1b D168V, respectively.Puri

15、ty: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Boceprevir.html Boceprevir HYPERLINK https:/www.MedChemE/Boceprevir.html HYPERLINK https:/www.MedChemE/boceprevir-d9.html Boceprevir-d9(EBP 520

16、; SCH 503034) Cat. No.: HY-10237 (EBP 520-d9; SCH 503034-d9) Cat. No.: HY-10237SBoceprevir (EBP 520) is a potent, highlyselective, orally bioavailable HCV NS3 proteaseinhibitor with a K of 14 nM in both enzyme assayiand an EC of 350 nM in cell-based replicon90assay. Boceprevir inhibits SARS-CoV-2 3C

17、Lproactivity.Boceprevir-d9 (EBP 520-d9) is the deuteriumlabeled Boceprevir. Boceprevir (EBP 520) is apotent, highly selective, orally bioavailable HCVNS3 protease inhibitor with a K of 14 nM in bothienzyme assay and an EC of 350 nM in cell-based90replicon assay.Purity: 97.81%Clinical Data: LaunchedS

18、ize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/ciluprevir.html Ciluprevir(BILN 2061; BILN 2061ZW) Cat. No.: HY-10242 HYPERLINK https:/www.MedC

19、hemE/Clemizole.html ClemizoleCat. No.: HY-30234Ciluprevir(BILN 2061) is a specific and potentpeptidomimetic inhibitor of the HCV NS3 proteasewith an IC of 3.0 nM.50Clemizole is an H1 histamine receptorantagonist, is found to substantially inhibit HCVreplication. Clemizole is an inhibitor of TRPC5cha

20、nnel. The IC of Clemizole for RNA binding by50NS4B is 241 nM, whereas its EC for viral50replication is 8 M.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Clemizole-hydrochloride.html Clemizole HYPERLIN

21、K https:/www.MedChemE/Clemizole-hydrochloride.html HYPERLINK https:/www.MedChemE/Clemizole-hydrochloride.html hydrochlorideCat. No.: HY-30234A HYPERLINK https:/www.MedChemE/coblopasvir.html Coblopasvir(KW-136) Cat. No.: HY-117411Clemizole hydrochloride is an H1 histaminereceptor antagonist, is found

22、 to substantiallyinhibit HCV replication. Clemizole hydrochlorideis an inhibitor of TRPC5 channel.Coblopasvir (KW-136) is a pangenotypicnon-structural protein 5A (NS5A) inhibitor.Coblopasvir can be used for research of chronichepatitis C virus infection.Purity: 99.99%Clinical Data: LaunchedSize: 10

23、mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/coblopasvir-dihydrochloride.html Coblopasvir HYPERLINK https:/www.MedChemE/coblopasvir-dihydrochloride.html HYPERLINK https:/www.MedChemE/coblopas

24、vir-dihydrochloride.html dihydrochloride(KW-136 dihydrochloride) Cat. No.: HY-117411A HYPERLINK https:/www.MedChemE/Danoprevir.html Danoprevir(ITMN-191; R7227; RO5190591; RG7227) Cat. No.: HY-10238Coblopasvir (KW-136) dihydrochloride is apangenotypic non-structural protein 5A (NS5A)inhibitor. Coblop

25、asvir dihydrochloride can be usedfor research of chronic hepatitis C virusinfection.Danoprevir (ITMN-191) is an orally active NS3/4Aprotease inhibitor for hepatitis C virus (HCV)with an IC of 0.29 nM and is selective for50NS3/4A over a panel of 53 proteases (IC higher50than 10 M).Purity: 98.45%Clini

26、cal Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.04%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/dehydrojuncusol.html Dehydrojuncusol HYPERLINK https:/www.MedChemE/dehydrojuncusol.html HYPERLINK https:/www.MedChem

27、E/faldaprevir.html FaldaprevirCat. No.: HY-N8188(BI 201335) Cat. No.: HY-15256Dehydrojuncusol, a potent HCV inhibitor, targetsHCV NS5A and is able to inhibit RNA replicationof replicons harboring resistance mutations toanti-NS5A direct-acting antivirals.Faldaprevir (BI 201335) is a potent, orally ac

28、tiveand selective noncovalent inhibitor of NS3/4Aprotease of HCV (hepatitis C virus) genotypes 1aand 1b, with K values of 2.6 and 2.0 nM,irespectively.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: Phase 3Size: 1 mg, 5 mg HYPERLINK https:/www.MedCh

29、emE/faldaprevir-d6.html Faldaprevir-d6 HYPERLINK https:/www.MedChemE/faldaprevir-d6.html HYPERLINK https:/www.MedChemE/Glecaprevir.html GlecaprevirCat. No.: HY-15256S(ABT-493) Cat. No.: HY-17634Faldaprevir-d6 is deuterium labeled Faldaprevir.Glecaprevir is a novel HCV NS3/4A proteaseinhibitor, with

30、IC values ranging from 3.5 to5011.3 nM. Glecaprevir is also a SARS-CoV 3CLproinhibitor with an IC of 4.09 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.M

31、edChemE/MK-5172.html Grazoprevir(MK-5172) Cat. No.: HY-15298 HYPERLINK https:/www.MedChemE/MK-5172-hydrate.html Grazoprevir HYPERLINK https:/www.MedChemE/MK-5172-hydrate.html HYPERLINK https:/www.MedChemE/MK-5172-hydrate.html hydrate(MK-5172 hydrate) Cat. No.: HY-15298BGrazoprevir (MK-5172) is a sel

32、ective inhibitor ofHepatitis C virus NS3/4a protease with broadactivity across genotypes and resistant variants,with Ks of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08inM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a),respectively.Grazoprevir hydrate (MK-5172 hydrate) is aselective inhibitor of Hepatitis C virus NS

33、3/4aprotease with broad activity across genotypes andresistant variants, with Ks of 0.01 nM (gt1b),i0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b),0.90 nM (gt3a), respectively.Purity: 99.98%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.10%Clinical Data: LaunchedSize:

34、10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/MK-5172-potassium-salt.html Grazoprevir HYPERLINK https:/www.MedChemE/MK-5172-potassium-salt.html HYPERLINK https:/www.MedChemE/MK-5172-potassium-salt.html potassium HYPERLINK https:/www.MedChemE/MK-5172-potassium-salt.html HYPERLI

35、NK https:/www.MedChemE/MK-5172-potassium-salt.html salt(MK-5172 potassium salt) Cat. No.: HY-15298A HYPERLINK https:/www.MedChemE/MK-5172-sodium-salt.html Grazoprevir HYPERLINK https:/www.MedChemE/MK-5172-sodium-salt.html HYPERLINK https:/www.MedChemE/MK-5172-sodium-salt.html sodium HYPERLINK https:

36、/www.MedChemE/MK-5172-sodium-salt.html HYPERLINK https:/www.MedChemE/MK-5172-sodium-salt.html salt(MK-5172 sodium salt) Cat. No.: HY-15298CGrazoprevir potassium salt (MK-5172 potassiumsalt) is a selective inhibitor of Hepatitis C virusNS3/4a protease with broad activity acrossgenotypes and resistant

37、 variants, with Ks of 0.01inM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM(gt2b), 0.90 nM (gt3a), respectively.Grazoprevir sodium salt (MK-5172 sodium salt) is aselective inhibitor of Hepatitis C virus NS3/4aprotease with broad activity across genotypes andresistant variants, with Ks of 0.01 nM (

38、gt1b),i0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b),0.90 nM (gt3a), respectively.Purity: 99.40%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/gsk2818713.html GSK2818713 HYPERLINK https:/www.MedChem

39、E/gsk2818713.html HYPERLINK https:/www.MedChemE/hcvp-in-1.html HCVP-IN-1Cat. No.: HY-145335 Cat. No.: HY-50680GSK2818713 is a novel Hepatitis C NS5Areplication complex inhibitor.HCVP-IN-1 (compound 1) is a hepatitis C viralpolymerase (HCVP) inhibitor.Purity: 98%Clinical Data: No Development Reported

40、Size: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html Hepatitis HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-

41、protease-inhibitor-2.html Virus HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html C HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/he

42、patitis-virus-c-ns3-protease-inhibitor-2.html NS3 HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html Protease HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html HYPERLI

43、NK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html Inhibitor HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-inhibitor-2.html 2 HYPERLINK https:/www.MedChemE/hepatitis-virus-c-ns3-protease-

44、inhibitor-2.html HYPERLINK https:/www.MedChemE/hz-1157.html HZ-1157Cat. No.: HY-P2502 Cat. No.: HY-109571Hepatitis Virus C NS3 Protease Inhibitor 2 is aproduct-based peptide inhibitor of hepatitis Cvirus (HCV) NS3 protease, with a K of 41 nM.iHZ-1157 inhibits HCV NS3/4A protease with anIC of 1.0 mol

45、/L. HZ-1157 (4a) has a high dengue50virus inhibitory activity (EC = 0.15 M) and is50a relatively nontoxic (CC 10 M) dengue50antiviral agent.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg

46、, 100 mg HYPERLINK https:/www.MedChemE/idx184.html IDX184 HYPERLINK https:/www.MedChemE/idx184.html HYPERLINK https:/www.MedChemE/isoeuphorbetin.html IsoeuphorbetinCat. No.: HY-19558 Cat. No.: HY-N7672IDX184 is a potent and orally bioavailableinhibitor of HCV replication. IDX184 potentlyinhibits HCV

47、 polymerase (IC =0.31 M, =52.350 KinM).Isoeuphorbetin, a dimeric coumarin isolated fromViola philippica, is a potent HCV proteaseinhibitor with an IC of 3.63 g/mL.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg4 Tel: 609-

48、228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Narlaprevir.html Narlaprevir(SCH 900518) Cat. No.: HY-10300 HYPERLINK https:/www.MedChemE/ns5a-in-1.html NS5A-IN-1Cat. No.: HY-145375Narlaprevir (SCH 900518) is a selective and orallybioavailable NS3 protease inhibitor wit

49、h a Kivalue of 6 nM and an EC value of 40 nM.90Narlaprevir also inhibits the HCV nonstructuralprotein 3 serine protease.NS5A-IN-1 is a prodrug of the HCV NS5A inhibitorPibrentasvir (ABT-530).Purity: 98.15%Clinical Data: Phase 3Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Develo

50、pment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ns5a-in-2.html NS5A-IN-2 HYPERLINK https:/www.MedChemE/ns5a-in-2.html HYPERLINK https:/www.MedChemE/ns5a-in-3.html NS5A-IN-3Cat. No.: HY-115981 Cat. No.: HY-115982NS5A-IN-2 (Compound 33) is a potent inhibitor ofNS5A. NS5A-IN-2 has extremel

51、y high potencyagainst HCV genotype 1b, improved activity againstgenotype 3a (GT 3a) and good metabolic stability.NS5A-IN-3 (Compound 15) is a potent inhibitor ofNS5A. NS5A-IN-3 has extremely high potencyagainst HCV genotype 1b, improved activity againstgenotype 3a (GT 3a) and good metabolic stabilit

52、y.NS5A-IN-3 exhibits a higher resistance barrierthan daclatasvir against genotype 1b.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/ns5a-in-4.html NS5A-IN-4Cat. No.: HY-146126 HYPERLINK

53、https:/www.MedChemE/Paritaprevir.html Paritaprevir(ABT-450; Veruprevir) Cat. No.: HY-12594NS5A-IN-4 (Compound 1.12) is an orally activepan-genotypic hepatitis C virus (HCV) NS5Ainhibitor with IC values of 1.2, 2296, 4.6, 362,5010.3 and 693 pM against gT1b, gT1a, gT2a,gT3a, gT4a and gT5a.Paritaprevir

54、 (ABT-450) is a potent non-structuralprotein 3/4A (NS3/4A) protease inhibitor withEC50s of 1 and 0.21 nM against HCV 1a and 1b,respectively. Paritaprevir is also a SARS-CoV3CLpro inhibitor with an IC of 1.31 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.89%Clinical

55、Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/samatasvir.html Samatasvir HYPERLINK https:/www.MedChemE/samatasvir.html HYPERLINK https:/www.MedChemE/Simeprevir.html Simeprevir(IDX719; IDX18719) Cat. No.: HY-16784 (TMC435) Cat. No.: HY-10241Samatasvir (IDX71

56、) is a potent, orally activeNS5A inhibitor of HCV replication. Samatasvir iseffective and selective against infectious HCV andreplicons, with EC s falling within a tight50range of 2 to 24 pM in genotype 1 through 5replicons.Simeprevir (TMC435) is an oral and potent HCVNS3/4A protease inhibitor with

57、a K of 0.36 nM.iSimeprevir inhibits HCV replication with an EC50of 7.8 nM. Simeprevir inhibits SARS-CoV-2 3CLproactivity.Purity: 99.39%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.46%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

58、 HYPERLINK https:/www.MedChemE/simeprevir-13cd3.html Simeprevir-13C,d3 HYPERLINK https:/www.MedChemE/simeprevir-13cd3.html HYPERLINK https:/www.MedChemE/Telaprevir.html Telaprevir(TMC435-13C,d3) Cat. No.: HY-10241S (VX-950) Cat. No.: HY-10235Simeprevir-13C,d3 (TMC435-13C,d3) is the 13C- anddeuterium

59、 labeled Simeprevir. Simeprevir (TMC435)is an oral and potent HCV NS3/4A proteaseinhibitor with a K of 0.36 nM. Simepreviriinhibits HCV replication with an EC of 7.8 nM.50Simeprevir inhibits SARS-CoV-2 3CLpro activity.Telaprevir (VX-950) is a highly selective,reversible, and potent peptidomimetic inhibitor ofthe HCV NS3-4A protease, the steady-stateinhibitory constant (K) of Telaprevir is 7 nMiagainst a genotype 1 (H strain) NS3 proteasedomain plus a NS4A cofactor peptide.Purity: 98%Clinical Data: No Developmen