HIV-Protease-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html HIV HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html ProteaseHIV protease, a homodimeric aspartyl protease, is crucial for the viral life-cycle, cleaving proviral polyproteins, hen

2、ce creatingmature protein components that are required for the formation of an infectious virus. HIV protease cleaves newly synthesizedpolyproteins at the appropriate places to create the mature protein components of an infectious HIV virion. HIV protease is acritical drug target in designing anti-r

3、etroviral drugs to treat HIV/AIDS (acquired immune deficiency syndrome).HIV-1 protease permits viral maturation by processing the Gag and Gag-Pro-Pol polyproteins. It recognizes and cleaves more than12 different substrates leading to viral maturation. Similar to that of HIV-1, HIV-2 protease is also

4、 a homodimeric aspartyl enzymethat plays a vital role in the HIV life-cycle through processing of Gag and Gag-Pro-Pol precursor polyproteins leading to viralmaturation.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html HIV HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html H

5、YPERLINK https:/www.MedChemE/Targets/HIV Protease.html Protease HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html HYPERLINK https:/www.MedChemE/Targets/HIV Protease.html Inhibitors HYPERLINK https:/www.MedChemE/20-21-dehydrolucidenic-acid-a.html 20(21)-Dehydrolucidenic HYPERLINK https:/www.Med

6、ChemE/20-21-dehydrolucidenic-acid-a.html HYPERLINK https:/www.MedChemE/20-21-dehydrolucidenic-acid-a.html acid HYPERLINK https:/www.MedChemE/20-21-dehydrolucidenic-acid-a.html HYPERLINK https:/www.MedChemE/20-21-dehydrolucidenic-acid-a.html ACat. No.: HY-N3502 HYPERLINK https:/www.MedChemE/Amprenavi

7、r.html Amprenavir(VX-478) Cat. No.: HY-1743020(21)-Dehydrolucidenic acid A is a triterpenoidisolated from the fruiting body of the fungusGanoderma sinense. 20(21)-Dehydrolucidenic acidA has weak anti-HIV-1 protease activity.Amprenavir (VX-478) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV

8、 infection.Amprenavir is also a SARS-CoV 3CLpro inhibitorwith an IC of 1.09 M.50Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.58%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/amprenavir-d4.html Amprenavir-d4Cat. No.: H

9、Y-17430S HYPERLINK https:/www.MedChemE/amprenavir-d4-1.html Amprenavir-d4-1(VX-478-d4-1) Cat. No.: HY-17430S1Amprenavir-d4 is the deuterium labeled Amprenavir.Amprenavir (VX-478) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.Amprenavir is also a SARS-CoV 3CLpro inhibitorwith an

10、IC of 1.09 M.50Amprenavir-d4-1 is deuterium labeled Amprenavir.Amprenavir (VX-478) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.Amprenavir is also a SARS-CoV 3CLpro inhibitorwith an IC50 of 1.09 M.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clin

11、ical Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atazanavir.html Atazanavir(BMS-232632) Cat. No.: HY-17367 HYPERLINK https:/www.MedChemE/Atazanavir-sulfate.html Atazanavir HYPERLINK https:/www.MedChemE/Atazanavir-sulfate.html HYPERLINK https:/www.MedChemE/Atazanavir-sulfate.html sulfate(BMS-

12、232632 sulfate) Cat. No.: HY-17367AAtazanavir (BMS-232632), a highly selective HIV-1protease inhibitor, is the first proteaseinhibitor approved for once-daily administration.Atazanavir (BMS-232632) is a substrate andinhibitor of CYP3A4, and an inhibitor and inducerof P-glycoprotein (P-gp).Atazanavir

13、 (BMS-232632) sulfate, a highlyselective HIV-1 protease inhibitor, is the firstprotease inhibitor approved for once-dailyadministration. Atazanavir sulfate is a substrateand inhibitor of CYP3A4, and an inhibitor andinducer of P-glycoprotein (P-gp).Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPu

14、rity: 99.94%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/atazanavir-d5.html Atazanavir-d5 HYPERLINK https:/www.MedChemE/atazanavir-d5.html HYPERLINK https:/www.MedChemE/atazanavir-d6.html Atazanavir-d6Cat. No.: HY-17367S3(BMS-232632-d6) Cat. No.: HY-173

15、67S4Atazanavir-d5 is the deuterium labeled Atazanavir.Atazanavir (BMS-232632), a highly selective HIV-1protease inhibitor, is the first proteaseinhibitor approved for once-daily administration.Atazanavir-d6 is deuterium labeled Atazanavir.Atazanavir (BMS-232632), a highly selective HIV-1protease inh

16、ibitor, is the first proteaseinhibitor approved for once-daily administration.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atazanavir-d9.html Atazanavir-d9 HYPERLINK https:/www.MedChe

17、mE/atazanavir-d9.html HYPERLINK https:/www.MedChemE/brecanavir.html Brecanavir(BMS-232632-d9) Cat. No.: HY-17367S2 (GW640385) Cat. No.: HY-121240Atazanavir-d9 (BMS-232632-d9) is the deuteriumlabeled Atazanavir. Atazanavir (BMS-232632), ahighly selective HIV-1 protease inhibitor, is thefirst protease

18、 inhibitor approved for once-dailyadministration.Brecanavir (GW640385) is a novel, potent HIVprotease inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesM

19、edChemE HYPERLINK https:/www.MedChemE/cytochalasin-a.html Cytochalasin HYPERLINK https:/www.MedChemE/cytochalasin-a.html HYPERLINK https:/www.MedChemE/cytochalasin-a.html ACat. No.: HY-N6773 HYPERLINK https:/www.MedChemE/Darunavir.html Darunavir(TMC114; UIC-94017) Cat. No.: HY-17040Cytochalasin A is

20、 a cell-permeable fungal toxinthat is an oxidized derivative of cytochalasin B.Cytochalasin A is an inhibitor of HIV-1 protease(IC =3 M) and inhibits actin polymerization and50interferes with microtubule assembly by reactingwith sulfhydryl groups.Darunavir (TMC114), an orally active nextgeneration H

21、IV protease inhibitor, has a similarantiviral activity against the mutant and thewild-type viruses.Purity: 99.02%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.84%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Darunavir-Ethanolate.html Da

22、runavir HYPERLINK https:/www.MedChemE/Darunavir-Ethanolate.html HYPERLINK https:/www.MedChemE/Darunavir-Ethanolate.html Ethanolate(TMC114 Ethanolate) Cat. No.: HY-17041 HYPERLINK https:/www.MedChemE/darunavir-d9.html Darunavir-d9(TMC114-d9; UIC-94017-d9) Cat. No.: HY-112585Darunavir ethanolate (TMC1

23、14 Ethanolate) is apotent HIV protease inhibitor used to treat andprevent HIV/AIDS. Darunavir has a K of 1 nM foriwild type HIV-1 protease.Darunavir-d9 (TMC114-d9) is the deuterium labeledDarunavir. Darunavir (TMC114), an orally activenext generation HIV protease inhibitor, has asimilar antiviral ac

24、tivity against the mutant andthe wild-type viruses.Purity: 99.81%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/DPC-681.html DPC-681(DPH-153893) Cat. No.: HY-19400 HYPERLINK https:/ww

25、w.MedChemE/escin-ia.html Escin HYPERLINK https:/www.MedChemE/escin-ia.html HYPERLINK https:/www.MedChemE/escin-ia.html IACat. No.: HY-N0554DPC-681 is a potent and selective inhibitor of HIVprotease with IC90s for wild-type HIV-1 of 4 to 40nM. IC50 value: 4 - 40 nM Target: HIV protease invitro: DPC 6

26、81 is extremely potent inhibitor ofwild-type HIV-1.Escin IA is a triterpene saponin isolated fromhorse chestnut, which inhibits HIV-1 protease withIC values of 35 M.50Purity: 99.89%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.74%Clinical Data: No Development

27、ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/ganoderic-acid-b.html Ganoderic HYPERLINK https:/www.MedChemE/ganoderic-acid-b.html HYPERLINK https:/www.MedChemE/ganoderic-acid-b.html acid HYPERLINK https:/www.MedChemE/ganoderic-acid-b.html HYPERLINK https:/www.MedChemE/ganoderic

28、-acid-b.html B HYPERLINK https:/www.MedChemE/ganoderic-acid-b.html HYPERLINK https:/www.MedChemE/ganodermanondiol.html GanodermanondiolCat. No.: HY-N2006 Cat. No.: HY-N2996Ganoderic acid B is a triterpene isolated from amushroom Ganoderma lucidum. Ganoderic acid Binhibits the activation of Epstein-B

29、arr virus(EBV) antigens as telomerase inhibitor. Ganodericacid B is a moderately active inhibitor againstHIV-1 protease.Ganodermanondiol is a melanogenesis inhibitorisolated from the Ganodermalucidum.Ganodermanondiol exhibits potentcytoprotective effects on tert-butylhydroperoxide-induced hepatotoxi

30、city.Purity: 99.31%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1.html HIV HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1.html HYPERLINK https:/www.MedChemE/hiv-protease-

31、substrate-1.html Protease HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1.html HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1.html Substrate HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1.html HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1.html 1 HYPERLINK https:/www.M

32、edChemE/hiv-protease-substrate-1.html HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html HIV HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html Protease HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tf

33、a.html HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html Substrate HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html 1 HYPERLINK https:/www.MedChemE/hiv-protease-substrate-1-tfa.html HYPERLINK https:/www.MedC

34、hemE/hiv-protease-substrate-1-tfa.html TFACat. No.: HY-P2344 Cat. No.: HY-P2344AHIV Protease Substrate 1, a fiuorogenic HIVprotease substrate, can be used to study enzymaticactivity of HIV protease.HIV Protease Substrate 1 TFA, a fiuorogenic HIVprotease substrate, can be used to study enzymaticactiv

35、ity of HIV protease.Purity: 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/hiv-1-protease-in-2.html HIV-1 HYPERLINK https:/www.MedChemE/hiv-1-protease-in-2.html HYPERLINK https:/ww

36、w.MedChemE/hiv-1-protease-in-2.html protease-IN-2Cat. No.: HY-146888 HYPERLINK https:/www.MedChemE/indinavir.html Indinavir(MK-639; L-735524) Cat. No.: HY-B0689HIV-1 protease-IN-2 is a potent HIV-1 proteaseinhibitor with an IC of 2.53 nM. HIV-150protease-IN-2 shows antiviral activity against DRV(Dar

37、unavir)-sensitive or DRV-resistant HIV-1variants.Indinavir(MK-639; L735524) is a potent andspecific HIV protease inhibitor that appears tohave good oral bioavailability.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https

38、:/www.MedChemE/indinavir-sulfate.html Indinavir HYPERLINK https:/www.MedChemE/indinavir-sulfate.html HYPERLINK https:/www.MedChemE/indinavir-sulfate.html sulfate(MK-639 sulfate; L735524 sulfate) Cat. No.: HY-B0689A HYPERLINK https:/www.MedChemE/indinavir-d6.html Indinavir-d6Cat. No.: HY-B0689SIndina

39、vir sulfate(MK-639 sulfate; L735524 sulfate) is a potent and specific HIV protease inhibitorthat appears to have good oral bioavailability.Indinavir sulfate is also a SARS-CoV 3CLproinhibitor with an IC of 1.71 M.50Indinavir-d6 is the deuterium labeled Indinavir.Indinavir (MK-639; L735524) is a pote

40、nt andspecific HIV protease inhibitor that appears tohave good oral bioavailability.Purity: 99.82%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/isoescin-ia.html Isoescin HYPERLINK https:/www.MedC

41、hemE/isoescin-ia.html HYPERLINK https:/www.MedChemE/isoescin-ia.html IA HYPERLINK https:/www.MedChemE/isoescin-ia.html HYPERLINK https:/www.MedChemE/L-689502.html L-689502Cat. No.: HY-N0556 Cat. No.: HY-U00261Isoescin IA is a triterpenoid saponin isolatedfrom the seeds of Aesculus chinensis. Isoesci

42、n IAhas anti-HIV-1 protease activity.L-689502 is a potent inhibitor of HIV-l proteasewith an IC of 1 nM.50Purity: 98.89%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/lopinavir.html Lopinavir HYPERLINK h

43、ttps:/www.MedChemE/lopinavir.html HYPERLINK https:/www.MedChemE/lopinavir-metabolite-m-1.html Lopinavir HYPERLINK https:/www.MedChemE/lopinavir-metabolite-m-1.html HYPERLINK https:/www.MedChemE/lopinavir-metabolite-m-1.html Metabolite HYPERLINK https:/www.MedChemE/lopinavir-metabolite-m-1.html HYPER

44、LINK https:/www.MedChemE/lopinavir-metabolite-m-1.html M-1(ABT-378) Cat. No.: HY-14588Cat. No.: HY-136703Lopinavir (ABT-378) is a highly potent, selectivepeptidomimetic inhibitor of the HIV-1 protease,with Ks of 1.3 to 3.6 pM for wild-type and mutantiHIV protease. Lopinavir acts by arrestingmaturati

45、on of HIV-1 thereby blocking itsinfectivity.Lopinavir Metabolite M-1, an active metabolite ofLopinavir, inhibits HIV protease with a K of 0.7ipM. Lopinavir Metabolite M-1 has antiviralactivities in vitro.Purity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg, 250 mgPurity: 98%Clinical

46、Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/lopinavir-d8.html Lopinavir-d8 HYPERLINK https:/www.MedChemE/lopinavir-d8.html HYPERLINK https:/www.MedChemE/nelfinavir.html NelfinavirCat. No.: HY-14588S1(AG1341) Cat. No.: HY-15287Lopinavir-d8 (ABT-378-d8) is the deuterium

47、 labeledLopinavir. Lopinavir (ABT-378) is a highly potent,selective peptidomimetic inhibitor of the HIV-1protease, with Ks of 1.3 to 3.6 pM for wild-typeiand mutant HIV protease.Nelfinavir (AG-1341) is a potent and orallybioavailable HIV-1 protease inhibitor (K=2 nM)ifor HIV infection. Nelfinavir is

48、 a broad-spectrum,anticancer agent.Purity: 98%Clinical Data: No Development ReportedSize: 1 mgPurity: 96.90%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Nelfinavir-Mesylate.html Nelfinavir HYPERLIN

49、K https:/www.MedChemE/Nelfinavir-Mesylate.html HYPERLINK https:/www.MedChemE/Nelfinavir-Mesylate.html Mesylate(AG 1343 Mesylate) Cat. No.: HY-15287A HYPERLINK https:/www.MedChemE/nelfinavir-d3.html Nelfinavir-d3Cat. No.: HY-15287SNelfinavir Mesylate (AG 1343 Mesylate) is a potentand orally bioavaila

50、ble HIV-1 protease inhibitor(K=2 nM) for HIV infection. Nelfinavir Mesylatei(AG 1343 Mesylate) is a broad-spectrum, anticanceragent.Nelfinavir-d3 (AG1341-d3) is the deuterium labeledNelfinavir. Nelfinavir (AG-1341) is a potent andorally bioavailable HIV-1 protease inhibitor (K=2inM) for HIV infectio

51、n. Nelfinavir is abroad-spectrum, anticancer agent.Purity: 99.07%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98%Clinical Data:Size: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/Pepstatin.html Pepstatin(Pepstatin A) Cat. No.: HY-P0018 HYPERLINK https:/www.MedChemE/

52、Pepstatin_Ammonium.html Pepstatin HYPERLINK https:/www.MedChemE/Pepstatin_Ammonium.html HYPERLINK https:/www.MedChemE/Pepstatin_Ammonium.html Ammonium(Pepstatin A Ammonium) Cat. No.: HY-P0018BPepstatin (Pepstatin A) is a specific asparticprotease inhibitor produced by actinomycetes,with IC s of 4.5

53、nM, 6.2 nM, 150 nM, 290 nM, 52050nM and 260 nM for hemoglobin-pepsin,hemoglobin-proctase, casein-pepsin,casein-proctase, casein-acid proteasePepstatin Ammonium is a specific aspartic proteaseinhibitor produced by actinomycetes, with IC s of504.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nMfor hemog

54、lobin-pepsin, hemoglobin-proctase,casein-pepsin, casein-proctase, casein-acidprotease and hemoglobin-acidPurity: 98.28%Clinical Data: No Development ReportedSize: 10 mg, 50 mgPurity: 99.76%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/Pepstatin_Trifluo

55、roacetate.html Pepstatin HYPERLINK https:/www.MedChemE/Pepstatin_Trifluoroacetate.html HYPERLINK https:/www.MedChemE/Pepstatin_Trifluoroacetate.html Trifluoroacetate(Pepstatin A Trifluoroacetate) Cat. No.: HY-P0018A HYPERLINK https:/www.MedChemE/PNU-103017.html PNU-103017Cat. No.: HY-19236Pepstatin

56、Trifluoroacetate (Pepstatin ATrifluoroacetate) is a specific aspartic proteaseinhibitor produced by actinomycetes, with IC s of504.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nMfor hemoglobin-pepsin, hemoglobin-proctase,casein-pepsin, casein-proctase,PNU-103017 is an HIV protease inhibitor.Purity:

57、99.11%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/Ritonavir.html Ritonavir HYPERLINK https:/www.MedChemE/Ritonavir.html HYPERLINK https:/www.MedChemE/ritonavir-13cd3.html Ritonavir

58、-13C,d3(ABT 538; RTV) Cat. No.: HY-90001 (ABT 538-13C,d3; RTV-13C,d3) Cat. No.: HY-90001S1Ritonavir (ABT 538) is an inhibitor of HIVprotease used to treat HIV infection and AIDS.Ritonavir is also a SARS-CoV 3CLpro inhibitorwith an IC of 1.61 M.50Ritonavir-13C,d3 (ABT 538-13C,d3) is the 13C- anddeute

59、rium labeled Ritonavir. Ritonavir (ABT 538)is an inhibitor of HIV protease used to treat HIVinfection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC of 1.61 M.50Purity: 99.95%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mgPurity: 98%Clinical Data: No Developm

60、ent ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ritonavir-d6.html Ritonavir-d6 HYPERLINK https:/www.MedChemE/ritonavir-d6.html HYPERLINK https:/www.MedChemE/rosamultin.html RosamultinCat. No.: HY-90001S Cat. No.: HY-N2565Ritonavir-d6 (ABT 538-d6) is the deuterium labeledRitonavir. Ritonav