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HIV mutants

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HIV (59) HIV Integrase (6) HIV Protease (11) Antibiotic (1) Cytochrome P450 (1) Drug Isomer (1) Fungal (1) Isotope-Labeled Compounds (8) MMP (2) Potassium Channel (2) Reference Standards (6) Reverse Transcriptase (28) SARS-CoV (7)
By Research Areas:	Cancer (4) Infection (59) Inflammation/Immunology (4) Neurological Disease (1)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: HIV Integrase HIV HIV Protease

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13238

Dolutegravir Maximum Cited Publications 32 Publications Verification S/GSK1349572	HIV Integrase HIV	Infection
Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-10574

Rilpivirine 5+ Cited Publications R278474; TMC278; DB08864	HIV Reverse Transcriptase	Infection
Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type *HIV* (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .

HY-14588

Lopinavir 15+ Cited Publications ABT-378	HIV HIV Protease SARS-CoV	Infection Neurological Disease Cancer
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-17040

Darunavir 15+ Cited Publications TMC114; UIC-94017	HIV HIV Protease	Infection Inflammation/Immunology
Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC₅₀ = 0.003 μM; IC₉₀ = 0.009 μM) with minimal cytotoxicity .

HY-16767

Doravirine 10+ Cited Publications MK-1439	HIV Reverse Transcriptase	Infection Inflammation/Immunology
Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC₅₀s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .

HY-13238A

Dolutegravir sodium Maximum Cited Publications 32 Publications Verification S/GSK1349572 sodium	HIV Integrase HIV	Infection
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-19851

Rovafovir etalafenamide GS-9131	Reverse Transcriptase HIV	Cancer
Rovafovir etalafenamide (GS-9131), a proagent of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity .

HY-10574A

Rilpivirine hydrochloride 5+ Cited Publications TMC-278 hydrochloride	SARS-CoV MMP	Infection
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type *HIV* (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .

HY-16767S1

Doravirine-13C,d3 MK-1439-¹³C,d₃	Isotope-Labeled Compounds HIV Reverse Transcriptase	Infection
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC₅₀s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .

HY-152161

HIV-1 inhibitor-51	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against *WT HIV-1 (IIIB)* and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (K_D=2.50 μM) and inhibitory activity (IC₅₀=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC₅₀s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .

HY-152160

HIV-1 inhibitor-50	HIV Reverse Transcriptase	Infection
HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC₅₀=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC₅₀s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains .

HY-175351

HIV-1-IN-83	HIV Reverse Transcriptase	Infection
HIV-1-IN-83 (Compound 18E) is a *HIV-1* non-nucleoside reverse transcriptase inhibitor with an IC₅₀ of 0.45 μM for wild-type HIV-1 non-nucleoside reverse transcriptase. HIV-1-IN-83 has potent antiviral activity against both HIV-1 wild-type and mutant strains and improves antidrug resistance for Y188L and RES056 mutant strains. HIV-1-IN-83 has no significant toxicity up to 11.088 μM .

HY-106918

Tivirapine R86183; TIBO R 86183	Reverse Transcriptase HIV	Infection
Tivirapine (R86183) is a nonnucleoside HIV-1 RT inhibitor against HIV-1-induced cytopathic effects with an EC₅₀ value of 4 nM. Tivirapine inhibits the Yl8lC mutant of HIV-1 RT .

HY-152560

HIV-1 inhibitor-55	HIV	Infection
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC₅₀ value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection .

HY-15352

BMS 561390 DPC 083	Reverse Transcriptase HIV	Infection
BMS 561390 (DPC 083) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains .

HY-174417

NNRT-IN-10	Reverse Transcriptase HIV Potassium Channel Cytochrome P450	Infection
NNRT-IN-10 is a potent, selective and orally active *non-nucleoside HIV-1 reverse transcriptase (NNRTI)* inhibitor with with an EC₅₀ values ranging from 1.16 to 18.3 nM for *HIV* and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1 .

HY-163110

NNRT-IN-2	HIV Reverse Transcriptase	Infection
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type *HIV-1* and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC₅₀ of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .

HY-171835

DPC 684	HIV HIV Protease	Infection
DPC 684 is a potent and selective HIV-1 protease inhibitor (IC₉₀ = 5.7-40 nM, Ki = 0.021 nM). DPC 684 competitively inhibits HIV-1 protease and blocks viral polyprotein cleavage. DPC 684 has low protein binding and broad-spectrum inhibition against a variety of wild-type and mutant HIV-1 proteases. DPC 684 has low protein binding and broad-spectrum inhibition (IC₉₀ = 1.9-6.3 nM). DPC 684 has research significance for HIV .

HY-130241

Reverse transcriptase-IN-1	HIV	Infection
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC₅₀ values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 III_B, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC₅₀of 13.7 nM against HIV-1 reverse transcriptase enzyme .

HY-14588S1

Lopinavir-d8	Isotope-Labeled Compounds HIV HIV Protease SARS-CoV	Infection
Lopinavir-d₈ (ABT-378-d₈) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 14.2 μM .

HY-178341

NNRT-IN-13	Reverse Transcriptase HIV	Infection
NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly inhibiting HIV-1 reverse transcriptase (IC₅₀ = 0.25 μM). NNRT-IN-13 exhibits excellent antiviral activity against wild-type *HIV-1* (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants. NNRT-IN-13 exhibits favorable in vivo metabolic and safety profiles. NNRT-IN-13 can be used for human immunodeficiency virus (HIV) research .

HY-175667

NNRT-IN-12	HIV Reverse Transcriptase	Infection
NNRT-IN-12 (compound 19) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor with an IC₅₀ value of 0.107 μM for WT HIV-1 RT. NNRT-IN-12 shows anti-HIV-1 activity with EC₅₀ value of 14.1, 5.03, 7.64, 27.1 nM for L100I, K103N, Y181C, Y188L mutant HIV-1 strains, respectively. NNRT-IN-12 shows cytotoxicity .

HY-13238S1

Dolutegravir-d3 S/GSK1349572-d₃	Isotope-Labeled Compounds HIV Integrase HIV	Infection
Dolutegravir-d₃ is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-13238S2

Dolutegravir-d5 S/GSK1349572-d₅	Isotope-Labeled Compounds HIV Integrase HIV	Infection
Dolutegravir-d₅ is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-13238R

Dolutegravir (Standard) S/GSK1349572 (Standard)	Reference Standards HIV Integrase HIV	Infection
Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-17040R

Darunavir (Standard) TMC114 (Standard); UIC-94017 (Standard)	HIV HIV Protease Reference Standards	Infection Inflammation/Immunology
Darunavir (Standard) is the analytical standard of Darunavir. This product is intended for research and analytical applications. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity .

HY-10574S

Rilpivirine-d6	Isotope-Labeled Compounds HIV Reverse Transcriptase	Infection
Rilpivirine-d₆ is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .

HY-118731

TNK-6123	Reverse Transcriptase	Infection
TNK-6123 is a potent Emivirine (HY-15353) analogue with improved activity against drug-resistant HIV mutants. TNK-6123 improves activity against Lys103Asn mutant RT .

HY-10574AR

Rilpivirine hydrochloride (Standard) TMC-278 hydrochloride (Standard); TMC278 hydrochloride (Standard); TMC 278 hydrochloride (Standard)	Reference Standards SARS-CoV MMP	Infection
Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .

HY-10574R

Rilpivirine (Standard) R278474 (Standard); TMC278 (Standard); DB08864 (Standard)	Reference Standards HIV Reverse Transcriptase	Infection
Rilpivirine (Standard) is the analytical standard of Rilpivirine. This product is intended for research and analytical applications. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .

HY-120331

U-89360E	HIV HIV Protease	Infection
U-89360E is an inhibitor for HIV-1 protease. U-89360E inhibits the protease of HIV-1 wildtype, V82D mutant and V82N mutant with K_i of 20 nM, 560 nM and 2100 nM, respectively .

HY-111079

HIV-1 inhibitor-70	HIV Reverse Transcriptase	Others
HIV-1 inhibitor-70 (compound 20) is a bifunctional inhibitor that inhibits both wild-type (WT) and K103N mutant reverse transcriptases (RTs) of HIV-1.

HY-175491

HIV-1-IN-85	HIV Reverse Transcriptase	Infection
HIV-1-IN-85 is an orally active *HIV-1* inhibitor (IC₅₀ = 72 nM). HIV-1-IN-85 exhibits strong inhibitory activity against wild-type (WT) *HIV-1* and NNRTI-resistant single mutant strains (L100I, K103N, Y181C, Y188L, E138K) and moderate efficacy against double mutant strains (F227L+V106A, RES056). HIV-1-IN-85 shows good in vivo safety in ICR mice. HIV-1-IN-85 can be used for the study of HIV-1 infection .

HY-151938

Reverse transcriptase-IN-3	HIV	Infection
Reverse transcriptase-IN-3 is a pyrimidine-5-carboxamide derivative, acts as an inhibitor of *HIV-1. Reverse transcriptase-IN-3 shows potent activity against the HIV-1* wild-type and mutant strains .

HY-155114

HIV-1 inhibitor-59	HIV	Infection
HIV-1 inhibitor-59 (Compound I-5b) is a *HIV-1* inhibitor, with EC₅₀s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC₅₀: 0.094-12.0 μM) .

HY-147841

HIV-1 inhibitor-41	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC₅₀ values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .

HY-167135

DPC-082	HIV Reverse Transcriptase	Infection
DPC-082 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of *HIV-1. DPC-082 inhibits wild-type RF virus with an IC₉₀ of 2.0 nM. DPC-082 inhibits various single and many multiple amino acid substituted HIV-1 mutant* viruses .

HY-162253

HIV-1 inhibitor-64	HIV	Infection
HIV-1 inhibitor-64 (Compound 7c) is a wild-type *HIV-1* inhibitor that effectively suppresses the activity of *HIV-1* mutants E138K/Q148K and G140S/Q148R with EC₅₀ values of 62.5 nM and 11.3 nM, respectively. HIV-1 inhibitor-64 exhibits antiviral activity and can be used in the research of AIDS .

HY-146746

HIV-1 inhibitor-19	HIV	Infection
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC₅₀s of 7.3 nM, 9.2 nM and 21.0 nM, respectively.

HY-178031

HIV-1-IN-87	HIV Reverse Transcriptase	Infection
HIV-1-IN-87 (Compound 11x) is a dual-site *HIV-1* inhibitor targeting the non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) and its adjacent site (NNIAS). HIV-1-IN-87 has potent antiviral activities against wild-type and mutant strains (such as L100I, K103N and Y181C) (EC₅₀: 4.1-150 nM). HIV-1-IN-87 can be used for HIV-1 infections like acquired immune deficiency syndrome (AIDS) research .

HY-172408

NNRT-IN-6	Reverse Transcriptase HIV	Infection
NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase (HIV-1 RT) with IC₅₀ of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC₅₀ of 6.2-250 nM .

HY-169920

HIV-1 inhibitor-79	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-79 (Compound 3k) is an *HIV* inhibitor that exhibits significant inhibitory activity against *HIV-1* and its common mutant strains (with IC₅₀ values of 1.9, 1.9, 8.7, and 11 nM against *HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC₅₀* = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against *HIV-2, with an EC₅₀* value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC₅₀ = 25 nM) .

HY-14588S2

Lopinavir-d7 ABT-378-d₇	HIV SARS-CoV HIV Protease Isotope-Labeled Compounds	Infection Cancer
Lopinavir-d₇ is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-14588R

Lopinavir (Standard) ABT-378 (Standard)	Reference Standards HIV HIV Protease SARS-CoV	Infection Cancer
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-146019A

HIV-1 inhibitor-25	HIV	Infection
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC₅₀ value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC₅₀ of 13.6 nM, and exhibits relatively low cytotoxicity with a CC₅₀ of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC₅₀ of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .

HY-14588S

(rel)-Lopinavir-d8 (rel)-ABT-378-d₈	Isotope-Labeled Compounds HIV Protease SARS-CoV HIV	Others
(rel)-Lopinavir-d₈ ((rel)-ABT-378-d₈) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-149928

NNRT-IN-1	HIV	Infection
NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC₅₀s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties .

HY-112585

Darunavir-d9 TMC114-d9; UIC-94017-d9	HIV HIV Protease	Infection Inflammation/Immunology
Darunavir-d9 (TMC114-d9) is the deuterium labeled Darunavir. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC₅₀ = 0.003 μM; IC₉₀ = 0.009 μM) with minimal cytotoxicity .

HY-162720

NNRT-IN-4	HIV Potassium Channel Reverse Transcriptase	Infection
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC₅₀ of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC₅₀ of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC₅₀=25.9 µM) and CYP enzymes (IC₅₀>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .

HY-152233

Reverse transcriptase-IN-4	HIV	Infection
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC₅₀ value of 0.053 μM for wild-type HIV-1 and an EC₅₀ value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Cat. No.	Product Name	Target	Research Area

HY-P5395

TAT-GluR23A Fusion Peptide	HIV	Others
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)

Cat. No.	Product Name	Chemical Structure

HY-16767S1

Doravirine-13C,d3
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC₅₀s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .

HY-14588S1

Lopinavir-d8

Lopinavir-d₈ (ABT-378-d₈) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 14.2 μM .

HY-13238S1

Dolutegravir-d3

Dolutegravir-d₃ is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-13238S2

Dolutegravir-d5

Dolutegravir-d₅ is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-10574S

Rilpivirine-d6
Rilpivirine-d₆ is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .

HY-14588S2

Lopinavir-d7

Lopinavir-d₇ is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-14588S

(rel)-Lopinavir-d8

(rel)-Lopinavir-d₈ ((rel)-ABT-378-d₈) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-10574S1

Rilpivirine-13C6

Rilpivirine- ¹³C₆ (R278474- ¹³C₆) is ¹³C labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .

Cat. No.	Product Name		Classification

HY-152233

Reverse transcriptase-IN-4		Azide
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC₅₀ value of 0.053 μM for wild-type HIV-1 and an EC₅₀ value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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