Search Result
Results for "
G��s Inhibitors
" in MedChemExpress (MCE) Product Catalog:
10
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-126303C
-
|
GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium
|
DNA/RNA Synthesis
SARS-CoV
RSV
HCV
Drug Metabolite
|
Infection
|
|
GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734) .
|
-
-
- HY-16593
-
|
|
HCV Protease
|
Infection
|
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GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity .
|
-
-
- HY-126303
-
|
GS-441524 triphosphate; Remdesivir metabolite
|
DNA/RNA Synthesis
SARS-CoV
RSV
HCV
Drug Metabolite
|
Infection
|
|
GS-443902 (GS-441524 triphosphate) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir .
|
-
-
- HY-129665
-
|
(±)-O,O-Dimethylcoclaurine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
GS 389 ((±)-O,O-Dimethylcoclaurine) is a tetrahydroisoquinoline. GS-389 inhibites Cyclic AMP and cyclic AMP dependent phosphodiesterases from rat atrial and ventricular tissue. GS-389 relaxes the contraction induced by phenylephrine and high K + in rat aortic rings .
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-
-
- HY-120159
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity .
|
-
-
- HY-15005
-
Sofosbuvir
Maximum Cited Publications
101 Publications Verification
GS-7977; PSI-7977
|
HCV
|
Infection
|
|
Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM .
|
-
-
- HY-137456
-
-
-
- HY-W394903
-
|
|
JAK
Drug Metabolite
|
Cancer
|
|
GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
|
-
-
- HY-15968
-
|
GS-9973
|
Syk
|
Cancer
|
|
Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC50 of 7.7 nM.
|
-
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
-
- HY-17605
-
-
-
- HY-12593
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.
|
-
-
- HY-109091
-
|
GS-9876
|
Syk
|
Inflammation/Immunology
|
|
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
|
-
-
- HY-19851
-
|
GS-9131
|
|
|
|
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-16727
-
|
GS-5806
|
RSV
|
Infection
|
|
Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM .
|
-
-
- HY-109091B
-
|
GS-9876 succinate
|
Syk
|
Inflammation/Immunology
|
|
Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
|
-
-
- HY-109091A
-
|
GS-9876 monosuccinate
|
Syk
|
Inflammation/Immunology
|
|
Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
|
-
-
- HY-17605S
-
|
|
Isotope-Labeled Compounds
|
Infection
|
|
Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
|
-
-
- HY-15232
-
|
GS-7340
|
HIV
Reverse Transcriptase
|
Infection
|
|
Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
|
-
-
- HY-15232A
-
|
GS-7340 fumarate
|
HIV
Reverse Transcriptase
|
Infection
|
|
Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
|
-
-
- HY-103586
-
|
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524, predominant metabolite of Remdesivir and superior to Remdesivir against Covid-19 , shows comparable efficacy in cell-based models of primary human lung and cat cells infected with coronavirus. GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM .
|
-
-
- HY-15232B
-
|
GS-7340 hemifumarate
|
HIV
Reverse Transcriptase
|
Infection
|
|
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
|
-
-
- HY-12633
-
|
|
HCV
|
Inflammation/Immunology
|
|
GS-6620 is?potent and selective pangenotype HCV inhibitor against HCV replicons of genotypes 1 to 6 (EC50: 0.048 to 0.68 μM). GS-6620 shows limited activities against other viruses, maintaining only some of its activity against the closely related bovine viral diarrhea virus (EC50, 1.5 μM) .
|
-
-
- HY-100844
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM .
|
-
-
- HY-100694
-
|
|
|
|
|
GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis .
|
-
-
- HY-W751039
-
|
GS-9883-d4
|
Isotope-Labeled Compounds
|
Infection
|
|
Bictegravir-d4 is a deuterium of Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
|
-
-
- HY-16901
-
|
ND-630; GS-0976; NDI-010976
|
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
|
-
-
- HY-138407
-
|
GS-4224; PD-1/PD-L1-IN 7
|
PD-1/PD-L1
HBV
|
Infection
Cancer
|
|
Evixapodlin (GS-4224) is a human PD-1/PD-L1 protein/protein interaction inhibitor with an IC50 of 0.213 nM. Evixapodlin has anticancer and antiviral functions .
|
-
-
- HY-110261
-
|
|
IKK
E1/E2/E3 Enzyme
NF-κB
|
Inflammation/Immunology
|
|
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect .
|
-
-
- HY-124594
-
|
GS-6207 analog
|
HIV
|
Infection
|
|
CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition . CA inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-18938
-
|
GS-4997
|
MAP3K
Apoptosis
|
Cancer
|
|
Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
|
-
-
- HY-17016
-
|
GS 4104 phosphate
|
Influenza Virus
|
Infection
|
|
Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
|
-
-
- HY-147264
-
|
GS-5718
|
IRAK
|
Inflammation/Immunology
|
|
Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research .
|
-
-
- HY-145994
-
|
ATV006
|
SARS-CoV
|
Infection
|
|
Obeldesivir (ATV006) is a potent, orally active antiviral agent and ester proagents of GS-441524. Obeldesivir inhibits the replication of SARS-CoV-2 and its variants. Obeldesivir can be used for SARS-CoV-2 research .
|
-
-
- HY-15602A
-
|
GS-5885 acetone
|
HCV
|
Infection
|
|
Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
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-
-
- HY-15602D
-
|
GS-5885 diacetone
|
HCV
|
Infection
|
|
Ledipasvir diacetone (GS-5885 diacetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
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-
-
- HY-114416
-
|
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Epigenetic Reader Domain
|
Cancer
|
|
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively .
|
-
-
- HY-15602
-
|
GS-5885
|
HCV
SARS-CoV
|
Infection
|
|
Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
|
-
-
- HY-15602C
-
|
GS-5885 hydrochloride
|
HCV
SARS-CoV
|
Infection
|
|
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
|
-
-
- HY-134557
-
|
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GSK-3
|
Cancer
|
|
GS87 is a highly specific and potent GSK3 inhibitor with IC50s of 415nM and 521nM for GSK3α and GSK3β, respectively. GS87 induces differentiation of acute myeloid leukemia (AML) cell lines by effectively activating GSK3-dependent signaling components including MAPK signaling. GS87 modulates key GSK3 target proteins involved in cell proliferation and differentiation more effectively than Lithium and SB415285 (SB). GS87 has the potential for acting as a differentiation agent for non-promyelocytic AML research .
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-
-
- HY-12530
-
|
GS-5816
|
HCV
SARS-CoV
|
Infection
Inflammation/Immunology
Cancer
|
|
Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
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-
-
- HY-14740
-
|
GS-9137; JTK-303; D06677
|
HIV Integrase
HIV
|
Infection
|
|
Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
|
-
-
- HY-13910
-
-
-
- HY-13026
-
|
CAL-101; GS-1101
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
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-
-
- HY-109050
-
|
GS-5829
|
Epigenetic Reader Domain
|
Cancer
|
|
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .
|
-
-
- HY-16750
-
|
GS-9669
|
HCV
|
Infection
|
|
Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM) .
|
-
-
- HY-15602S
-
|
GS-5885-d6
|
HCV
SARS-CoV
|
Infection
|
|
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
|
-
-
- HY-14740S
-
|
GS-9137-d8; JTK-303-d8; D06677-d8
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
|
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
|
-
-
- HY-10493S
-
|
GS-9350-d8
|
Isotope-Labeled Compounds
HIV
Cytochrome P450
|
Infection
|
|
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
|
-
-
- HY-19840
-
|
GS-9857
|
HCV Protease
|
Infection
|
|
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively . Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research .
|
-
- HY-155488
-
|
ATV014
|
SARS-CoV
|
Infection
|
|
SHEN26 (ATY014) is a potent and orally active RdRp inhibitor, with an IC50 for SARS-CoV-2 is 1.36 μM. SHEN26 is a 5’-cyclohexanecarboxylate derivative of GS-441524 (HY-103586). SHEN26 inhibits viral nucleic acid synthesis to achieve antiviral effects. SHEN26 can be used for the research of coronavirus disease 2019 (COVID-19) .
|
-
- HY-17016S1
-
|
GS 4104-d3 phosphate
|
Isotope-Labeled Compounds
Influenza Virus
|
Infection
|
|
Oseltamivir-d3 (phosphate)eis the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
|
-
- HY-B1826
-
|
GS-0393; PMEA
|
HBV
Reverse Transcriptase
|
Infection
|
|
Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses .
|
-
- HY-17016S
-
|
GS 4104-d5 phosphate
|
Isotope-Labeled Compounds
Influenza Virus
|
Infection
|
|
Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B[1][2].
|
-
- HY-17016R
-
|
GS 4104 phosphate (Standard)
|
Influenza Virus
|
Infection
|
|
Oseltamivir (phosphate) (Standard) is the analytical standard of Oseltamivir (phosphate). This product is intended for research and analytical applications. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
|
-
- HY-W074930
-
|
(S)-GS 1278; (S)-PMPA; (S)-TDF
|
HIV
HBV
|
Infection
|
|
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV) .
|
-
- HY-112461A
-
|
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
|
-
- HY-14391
-
|
GS-558093
|
HCV
|
Infection
|
|
PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes .
|
-
- HY-113904S
-
|
|
Reverse Transcriptase
HIV
HBV
|
Infection
|
|
(Rac)-Tenofovir-d6 is a labelled racemic Tenofovir. Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].
|
-
- HY-162008
-
|
|
HSP
Bcl-2 Family
|
Cancer
|
|
S1g-10 is a Hsp70/Bim inhibitor, and shows antitumor activity in chronic myeloid leukemia cells .
|
-
- HY-B1826S2
-
|
GS-0393-d4; PMEA-d4
|
HBV
Reverse Transcriptase
|
Infection
|
|
Adefovir-d4 is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
|
-
- HY-13318
-
|
GS 4071; Ro 64-0802; Oseltamivir carboxylate
|
Influenza Virus
Drug Metabolite
|
Infection
|
|
Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-111964
-
|
GS-6207
|
HIV
|
Infection
|
|
Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs) . Lenacapavir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17438
-
|
GS 0504; HPMPC; (S)-HPMPC
|
CMV
Apoptosis
DNA/RNA Synthesis
Orthopoxvirus
Endogenous Metabolite
|
Infection
Cancer
|
|
Cidofovir (GS 0504) is an acyclic monophosphate nucleotide analogue and CMV inhibitor with antiviral activity. Cidofovir inhibits cytomegalovirus (CMV) replication by selectively inhibiting viral DNA polymerase. Cidofovir induces apoptosis and can be used in studies of AIDS cytomegalovirus retinitis, herpes, and cancer . Cidofovir also has anti-orthopoxvirus and anti-variola activities .
|
-
- HY-16738A
-
|
GS 6615 hydrochloride
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
|
Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias .
|
-
- HY-17438A
-
|
GS 0504 dihydrate; HPMPC dihydrate; (S)-HPMPC dihydrate
|
CMV
DNA/RNA Synthesis
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Cidofovir (GS 0504; HPMPC; (S)-HPMPC) dihydrate is an acyclic monophosphate nucleotide analogue and CMV inhibitor with antiviral activity. Cidofovir dihydrate inhibits cytomegalovirus (CMV) replication by selectively inhibiting viral DNA polymerase. Cidofovir dihydrate induces apoptosis and can be used in studies of AIDS cytomegalovirus retinitis, herpes, and cancer . Cidofovir dihydrate also has anti-orthopoxvirus and anti-variola activities .
|
-
- HY-13317
-
|
GS 4104
|
Influenza Virus
|
Infection
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Oseltamivir (GS 4104) is an orally active influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC50s of 0.67, 0.9, 1.34 and 13 nM, respectively .
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- HY-P1376A
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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- HY-151441
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LRRK2
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Neurological Disease
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LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier .
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- HY-151444
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LRRK2
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Neurological Disease
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LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier .
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- HY-13318S1
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GS 4071-13C,d3; Ro 64-0802-13C,d3; Oseltamivir carboxylate-13C,d3
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Isotope-Labeled Compounds
Drug Metabolite
Influenza Virus
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Infection
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Oseltamivir acid-13C,d3 (GS 4071-13C,d3; Ro 64-0802-13C,d3) is a 13C- and deuterium-labeled Oseltamivir acid (HY-13318). Oseltamivir acid is the active metabolite of Oseltamivir phosphate and inhibits influenza virus neuraminidase (IC50=2 nM). Oseltamivir acid is orally active and can be used to study influenza A/B infections .
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- HY-146677
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5-HT Receptor
Monoamine Oxidase
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Neurological Disease
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5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT6R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits . 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1376A
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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- HY-P1376
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-15602S
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Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
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- HY-17605S
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Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
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- HY-W751039
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Bictegravir-d4 is a deuterium of Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
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- HY-14740S
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Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
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- HY-10493S
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Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
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- HY-17016S1
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Oseltamivir-d3 (phosphate)eis the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
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- HY-17016S
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Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B[1][2].
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- HY-113904S
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(Rac)-Tenofovir-d6 is a labelled racemic Tenofovir. Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].
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- HY-B1826S2
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Adefovir-d4 is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
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- HY-13318S1
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Oseltamivir acid-13C,d3 (GS 4071-13C,d3; Ro 64-0802-13C,d3) is a 13C- and deuterium-labeled Oseltamivir acid (HY-13318). Oseltamivir acid is the active metabolite of Oseltamivir phosphate and inhibits influenza virus neuraminidase (IC50=2 nM). Oseltamivir acid is orally active and can be used to study influenza A/B infections .
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| Cat. No. |
Product Name |
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Classification |
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- HY-146677
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Alkynes
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5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT6R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits . 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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