HIV-Integrase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html HIV HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html IntegraseHIV integrase is one of the three key enzymes of the pol gene of HIV. HIV integrase catalyzes the insertion into th

2、e genome of theinfected human cell of viral DNA produced by the retrotranscription process. This unique step in the virus life cycle provides avariety of points for intervention and hence is an attractive target for the development of new therapeutics for the treatment ofAIDS. HIV integrase includes

3、 HIV-1 and HIV-2 integrases.HIV-1 integrase is a 32-kDa enzyme that carries out DNA integration in a two-step reaction. In the first step, called 3 processing,two nucleotides are removed from each 3 end of the viral DNA made by reverse transcription. In the next step, called DNA strandtransfer, a pa

4、ir of transesterification reactions integrates the ends of the viral DNA into the host genome. Integrase is comprised ofthree structurally and functionally distinct domains, and all three domains are required for each step of the integration reaction.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targ

5、ets/HIV Integrase.html HIV HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html Integrase HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html HYPERLINK https:/www.MedChemE/Targets/HIV Integrase.html Inhibitors HYPERLINK https:/www.Med

6、ChemE/s-bi-1001.html (S)-BI-1001 HYPERLINK https:/www.MedChemE/s-bi-1001.html HYPERLINK https:/www.MedChemE/_plusmn_-BI-D.html ()-BI-DCat. No.: HY-12210 Cat. No.: HY-18601(S)-BI-1001 (Compound 11) is an activeS-enantiomer of BI-1001. (S)-BI-1001 exhibitsantiviral potency against HIV-1 integrase with

7、 anIC50 of 28 nM, an EC50 of 450 nM and a Kd of4.7 M.()-BI-D is a potent ALLINI(An allosteric INinhibitor) that binds integrase at the LEDGF/p75binding site.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.02%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

8、 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BI-224436.html BI HYPERLINK https:/www.MedChemE/BI-224436.html HYPERLINK https:/www.MedChemE/BI-224436.html 224436Cat. No.: HY-18595 HYPERLINK https:/www.MedChemE/Bictegravir.html Bictegravir(GS-9883) Cat. No.: HY-17605BI 224436 is a novel HIV-1 nonca

9、talytic siteintegrase inhibitor with EC values of less50than 15 nM against different HIV-1 laboratorystrains.Bictegravir (GS-9883) is a potent inhibitor ofHIV-1 integrase with an IC of 7.5 nM.50Purity: 99.74%Clinical Data: Phase 1Size: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.88%Clinical Data: LaunchedS

10、ize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BMS-707035.html BMS-707035Cat. No.: HY-13269 HYPERLINK https:/www.MedChemE/Cabotegravir.html Cabotegravir(GSK-1265744; S/GSK1265744) Cat. No.: HY-15592BMS-707035 is an HIV-1 integrase (IN) inhibitorwith an IC50 value of

11、15 nM.Cabotegravir is a potent HIV integrase inhibitoras an oral lead-in tablet and long-actinginjectable for the treatment and prevention of HIVinfection. Cabotegravir is an inhibitor of OAT1(IC50 0.81 M) and OAT3 (IC50 0.41 M).Purity: 99.50%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5

12、 mg, 10 mg, 50 mg, 100 mgPurity: 98.04%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/cabotegravir-d3.html Cabotegravir-d3 HYPERLINK https:/www.MedChemE/cabotegravir-d3.html HYPERLINK https:/www.MedChemE/cabotegravir-d5.html Cabotegravir-d5(GSK-1265744-d3;

13、 S/GSK1265744-d3) Cat. No.: HY-15592S (GSK-1265744-d5; S/GSK1265744-d5) Cat. No.: HY-15592S1Cabotegravir-d3 (GSK-1265744-d3) is the deuteriumlabeled Cabotegravir. Cabotegravir is a potent HIVintegrase inhibitor as an oral lead-in tablet andlong-acting injectable for the treatment andprevention of HI

14、V infection.Cabotegravir-d5 is deuterium labeled Cabotegravir.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/Dolutegravir.html Dolutegravir HYPERLINK https:/www.MedChemE/Dolutegravir.htm

15、l HYPERLINK https:/www.MedChemE/Dolutegravir-sodium.html Dolutegravir HYPERLINK https:/www.MedChemE/Dolutegravir-sodium.html HYPERLINK https:/www.MedChemE/Dolutegravir-sodium.html sodium(S/GSK1349572) Cat. No.: HY-13238 (S/GSK1349572 sodium) Cat. No.: HY-13238ADolutegravir (S/GSK1349572) is a highly

16、 potent andorally bioavailable HIV integrase strand transferinhibitor with an IC of 2.7 nM for HIV-150integrase-catalyzed strand transfer.Dolutegravir sodium (S/GSK1349572 sodium) is ahighly potent and orally bioavailable HIV integrasestrand transfer inhibitor with an IC of 2.7 nM50for HIV-1 integra

17、se-catalyzed strand transfer.Purity: 99.65%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.88%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/

18、dolutegravir-d3.html Dolutegravir-d3(S/GSK1349572-d3) Cat. No.: HY-13238S1 HYPERLINK https:/www.MedChemE/dolutegravir-d5.html Dolutegravir-d5(S/GSK1349572-d5) Cat. No.: HY-13238S2Dolutegravir-d3 (S/GSK1349572-d3) is the deuteriumlabeled Dolutegravir. Dolutegravir (S/GSK1349572)is a highly potent and

19、 orally bioavailable HIVintegrase strand transfer inhibitor with an IC50of 2.7 nM for HIV-1 integrase-catalyzed strandtransfer.Dolutegravir-d5 is deuterium labeled Dolutegravir.Dolutegravir (S/GSK1349572) is a highly potent andorally bioavailable HIV integrase strand transferinhibitor with an IC50 o

20、f 2.7 nM for HIV-1integrase-catalyzed strand transfer.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/dolutegravir-d6-sodium.html Dolutegravir-d6 HYPERLINK https:/www.MedChemE/dolutegravi

21、r-d6-sodium.html HYPERLINK https:/www.MedChemE/dolutegravir-d6-sodium.html sodium(S/GSK1349572-d6 sodium) Cat. No.: HY-13238AS HYPERLINK https:/www.MedChemE/Elvitegravir.html Elvitegravir(GS-9137; JTK-303; D06677) Cat. No.: HY-14740Dolutegravir-d6 sodium (S/GSK1349572-d6 sodium) isthe deuterium labe

22、led Dolutegravir sodium.Elvitegravir (GS-9137; JTK-303; D06677) is an HIVintegrase inhibitor for HIV-1 , HIV-2 andIIIB EHOHIV-2 with of 0.7 nM, 2.8 nM and 1.4 nM,respectively.ROD IC50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.85%Clinical Data: LaunchedSize: 10 mM 1 m

23、L, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/elvitegravir-d8.html Elvitegravir-d8(GS-9137-d8; JTK-303-d8; D06677-d8) Cat. No.: HY-14740S HYPERLINK https:/www.MedChemE/equisetin.html EquisetinCat. No.: HY-N6711Elvitegravir-d8 is deuterium labeled Elvitegravir.Elvitegravir (GS-9137; JTK-303;

24、D06677) is an HIVintegrase inhibitor for HIV-1IIIB, HIV-2EHO andHIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM,respectively.Equisetin is an N-methylserine-derived acyltetramic acid isolated from a terrestrial fungusFusarium equiseti NRRL 5537. Equisetin is atetramate-containing natural product with

25、antibiotic and cytotoxic activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.12%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor.html HIV-1 HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor.ht

26、ml HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor.html integrase HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor.html HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor.html inhibitor HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor.html HYPERLINK https:/www.MedChemE/HIV

27、-1_integrase_inhibitor_3.html HIV-1 HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_3.html HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_3.html integrase HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_3.html HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_3.html in

28、hibitor HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_3.html HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_3.html 3Cat. No.: HY-13025 Cat. No.: HY-108817HIV-1 integrase inhibitor is uesful for anti-HIV.HIV-1 integrase inhibitor 3 is a HIV-1 integrasestrand transfer (INST) inhibit

29、or with an IC of502.7 nM.Purity: 96.37%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 https:/www.MedChemE/HIV-1_integrase_inhibitor_4.html HIV-1 HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhi

30、bitor_4.html HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_4.html integrase HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_4.html HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_4.html inhibitor HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_4.html HYPERLINK https

31、:/www.MedChemE/HIV-1_integrase_inhibitor_4.html 4 HYPERLINK https:/www.MedChemE/HIV-1_integrase_inhibitor_4.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-7.html HIV-1 HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-7.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor

32、-7.html integrase HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-7.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-7.html inhibitor HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-7.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-7.html 7Cat. No.: HY-108820

33、 Cat. No.: HY-130760HIV-1 integrase inhibitor 4 is a HIV-1 integrasestrand transfer (INST) inhibitor with an IC of503.7 nM.HIV-1 integrase inhibitor 7 is a potent HIV-1integrase inhibitor, with an IC of 33.3 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Da

34、ta: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html HIV-1 HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html integrase HYPERLINK https:/www.MedChemE/hiv-1-i

35、ntegrase-inhibitor-8.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html inhibitor HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html 8 HYPERLINK https:/www.MedChemE/hiv-1-integrase-inhibitor-8.html HYPERLINK

36、https:/www.MedChemE/integracin-b.html Integracin HYPERLINK https:/www.MedChemE/integracin-b.html HYPERLINK https:/www.MedChemE/integracin-b.html BCat. No.: HY-107485 Cat. No.: HY-N7330HIV-1 integrase inhibitor 8 is a HIV-1 integraseinhibitor, compound 8.Integracin B is a potent dimeric alkyl aromati

37、cinhibitor of HIV-1 integrase discovered from thescreening of fungal extracts using an in vitroassay. Integracin B inhibits both coupled andstrand transfer activity of HIV-1 integrase.Purity: 99.88%Clinical Data: No Development ReportedSize: 50 mg, 100 mgPurity: 98%Clinical Data: No Development Repo

38、rtedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/L-Chicoric-Acid.html L-Chicoric HYPERLINK https:/www.MedChemE/L-Chicoric-Acid.html HYPERLINK https:/www.MedChemE/L-Chicoric-Acid.html Acid(-)-Chicoric acid; trans-Caffeoyltartaric acid) Cat. No.: HY-N0457A HYPERLINK https:/www.MedChemE/lavendustin-b

39、.html Lavendustin HYPERLINK https:/www.MedChemE/lavendustin-b.html HYPERLINK https:/www.MedChemE/lavendustin-b.html BCat. No.: HY-108935L-Chicoric Acid (-)-Chicoric acid) is adicaffeoyltartaric acid and a potent, selectiveand reversible HIV-1 integrase inhibitor with anIC50 of 100 nM. L-Chicoric Aci

40、d inhibits HIV-1replication in tissue culture.Lavendustin B is an inhibitor of HIV-1 integraseinteraction with LEDGF/p75 with an IC of 94.0750M. Lavendustin B is an ATP-competitive GLUT1inhibitor with a K of 15 M. Lavendustin B isialso a weak inhibitor of tyrosine kinases.Purity: 99.98%Clinical Data

41、: No Development ReportedSize: 10 mgPurity: 98.04%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/HIV-1-integrase-inhibitor-2.html LEDGIN6(CX05168; CX04328) Cat. No.: HY-10522 HYPERLINK https:/www.MedChemE/mk-2048.html MK-2048Ca

42、t. No.: HY-13305LEDGIN6 (CX05168) is a quinoline-basedprotein-protein interaction inhibitor ofLEDGF/p75 and HIV integrase.MK-2048 is a potent inhibitor of integrase andINR263K with IC50 of 2.6 nM and 1.5 nM,respectively. IC50 Value: 2.6 nM for HIV IntegraseTarget: HIV Integrase MK-2048 is a secondge

43、neration integrase inhibitor, intended to beused against HIV infection.Purity: 98.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.0%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pirmitegravir.html Pirmitegravir HYPERLINK https:/www.MedCh

44、emE/pirmitegravir.html HYPERLINK https:/www.MedChemE/raltegravir.html RaltegravirCat. No.: HY-130000(MK-0518) Cat. No.: HY-10353Pirmitegravir is a potent and first-in-classinhibitor of allosteric integrase (ALLINI) thattargets LEDGF/p75 binding site. Pirmitegravirdisplays picomolar IC in human PBMCs

45、 with a5024,000 therapeutic index against HIV-1.Raltegravir is a potent integrase (IN) inhibitor,used to treat HIV infection.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.53%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Ralteg

46、ravir-potassium-salt.html Raltegravir HYPERLINK https:/www.MedChemE/Raltegravir-potassium-salt.html HYPERLINK https:/www.MedChemE/Raltegravir-potassium-salt.html potassium HYPERLINK https:/www.MedChemE/Raltegravir-potassium-salt.html HYPERLINK https:/www.MedChemE/raltegravir-d3-potassium-salt.html Raltegravir-d3 HYPERLINK https:/www.MedChemE/raltegravir-d3-potassium-salt.html HYPERLINK https:/www.MedChemE/raltegravir-d3-potassium-salt.html potassium(MK 0518 potassium) Cat. No.: HY-10353A (M