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Pathways Recommended: Metabolic Enzyme/Protease
Results for "

good metabolic stability

" in MedChemExpress (MCE) Product Catalog:

50

Inhibitors & Agonists

1

Screening Libraries

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150719
    AIMP2-DX2-IN-1

    		Others Cancer
    AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM .
    AIMP2-DX2-IN-1
  • HY-155992
    WLB-89462

    		Sigma Receptor Neurological Disease
    WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
    WLB-89462
  • HY-146120
    Antitubercular agent-25

    		Bacterial Infection
    Antitubercular agent-25 (Compound 28) is an anti-tubercular agent with an extracellular IC50 of 0.42 μM and an intracellular IC50 of 0.20 μM against M. tuberculosis H37Rv. Antitubercular agent-25 exhibits good metabolic stability .
    Antitubercular agent-25
  • HY-149339
    hnNOS-IN-2

    		NO Synthase Neurological Disease
    hnNOS-IN-2 (compound 17) is a human neuronal nitric oxide synthase (hnNOS) inhibitor with good metabolic stability. hnNOS-IN-2 can be used for research in neurodegenerative diseases .
    hnNOS-IN-2
  • HY-163751
    STING-IN-9

    		Mineralocorticoid Receptor Metabolic Disease
    STING-IN-9 (compound 2) is a potent inhibitor of human CYP11B2. STING-IN-9 showed more than 80 times higher selectivity over human CYP11B1 in vitro .
    STING-IN-9
  • HY-161993
    BI-9787

    		Ketohexokinase Metabolic Disease
    BI-9787 is a zwitterionic inhibitior for ketohexokinase, with an IC50 of 12 and 12.8 nM for hKHK-A and hKHK-C. BI-9787 exhibits good metabolic stability in rat hepatocyte and good pharmacokinetic characteristics in rats .
    BI-9787
  • HY-151200
    Steroid sulfatase-IN-4

    		Steroid Sulfatase Endocrinology
    Steroid sulfatase-IN-4 (Compound 16) is an irreversible steroid sulfatase (STS) inhibitor with an IC50 of 25 nM against human STS. Steroid sulfatase-IN-4 can be used for the research of endometriosis .
    Steroid sulfatase-IN-4
  • HY-120454
    G-479

    		MEK Potassium Channel Cancer
    G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
    G-479
  • HY-167856
    RTI-122

    		GPR88 Neurological Disease
    RTI-122 is a brain-penetrant and potent GPR88 agonist with good metabolic stability (half-life of 5.8 h in mice) and a cAMP EC50 of 11 nM. RTI-122 can be utilized in research on excessive drinking .
    RTI-122
  • HY-169258
    PDE4-IN-21

    		Phosphodiesterase (PDE) Metabolic Disease
    PDE4-IN-21 (Compound L19) is a poetent PDE4 inhibitor, with an IC50 of 0.48 μM. PDE4-IN-21 exhibits good inhibitory activity and remarkable metabolic stability in rat liver microsomes .
    PDE4-IN-21
  • HY-153822
    JG-23

    		Tau Protein Neurological Disease
    JG-23 is a 4-chloro modified analog with ability to promote t-tau degradation. JG-23 exhibits good metabolic stability with a long T1/2 value (36 min) in mouse liver microsome assays .
    JG-23
  • HY-162928
    RIPK1-IN-26

    		Ser/Thr Protease Neurological Disease
    RIPK1-IN-26 (Compound 8a) is a potent receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitor with cell anti-necroptosis potency. RIPK1-IN-26 demonstrats good metabolic stability and good binding specificity in mice. RIPK1-IN-26 is promising for research of PET imaging probe development and neurodegenerative disorders .
    RIPK1-IN-26
  • HY-147657
    GABAA receptor modulator-2

    		GABA Receptor Neurological Disease
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
    GABAA receptor modulator-2
  • HY-146268
    CaMKIIα-IN-1

    		CaMK Neurological Disease
    CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability .
    CaMKIIα-IN-1
  • HY-149242
    MAO-B-IN-20

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease .
    MAO-B-IN-20
  • HY-145713
    GS-8873

    HBV-IN-19

    		 HBV Infection
    GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
    GS-8873
  • HY-146121
    Antitubercular agent-26

    		Bacterial Infection
    Antitubercular agent-26 (Compound 32) is an orally active anti-tubercular agent with an extracellular IC50 of 0.50 μM and an intracellular IC50 of 0.51 μM against M. tuberculosis H37Rv. Antitubercular agent-26 shows good metabolic stability, low risk of cardiotoxicity and no genotoxicity .
    Antitubercular agent-26
  • HY-120398
    CH5447240

    		PTHR Endocrinology
    CH5447240 is an agonist for parathyroid hormone receptor 1 (PTHR1), that inhibits human PTHR1 with an EC50 of 12 μM. CH5447240 exhibits good metabolic stability in human liver microsomes. CH5447240 increases serum calcium levels in rats. CH5447240 can be used in research about hypoparathyroidism .
    CH5447240
  • HY-155538
    Cisd2 agonist 1

    		Others Metabolic Disease
    Cisd2 agonist 1 (Compound 4q) is a Cisd2 agonist (EC50: 34 nM). Cisd2 agonist 1 enhances the Cisd2 expression and improves the pathological changes in the fatty livers. Cisd2 agonist 1 has good metabolic stability. Cisd2 agonist 1 can be used for research of NAFLD .
    Cisd2 agonist 1
  • HY-160656
    5-HT/NA Reuptake inhibitor-1

    		5-HT Receptor Neurological Disease
    5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
    5-HT/NA Reuptake inhibitor-1
  • HY-159895
    PAR4 antagonist 7

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice .
    PAR4 antagonist 7
  • HY-158316
    BTL-MK

    		Others Others
    BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumins (HY-W250978)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
    BTL-MK
  • HY-159091
    HIV-1 integrase inhibitor 12

    		HIV Integrase Infection
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
    HIV-1 integrase inhibitor 12
  • HY-143330
    MAO-B-IN-4

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
    MAO-B-IN-4
  • HY-101930A
    (Rac)-BMS-816336

    		11β-HSD Metabolic Disease
    (Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of human and mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability .
    (Rac)-BMS-816336
  • HY-107460
    LDN-211904 oxalate

    		Ephrin Receptor Cancer
    LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC .
    LDN-211904 oxalate
  • HY-152468
    Antitumor agent-83

    		Apoptosis Cancer
    Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
    Antitumor agent-83
  • HY-160023
    D3S-001

    		Ras Cancer
    D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    D3S-001
  • HY-144632
    Antifungal agent 22

    		Fungal Infection
    Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .
    Antifungal agent 22
  • HY-147754
    JAK3/BTK-IN-6

    		Btk JAK Inflammation/Immunology
    JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
    JAK3/BTK-IN-6
  • HY-146594
    NLRP3-IN-8

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM) .
    NLRP3-IN-8
  • HY-146388
    Mtb ATP synthase-IN-1

    		Bacterial ATP Synthase Infection
    Mtb ATP synthase-IN-1 (compound 6ab) is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC50 > 64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium .
    Mtb ATP synthase-IN-1
  • HY-146617
    GLS1 Inhibitor-4

    		Glutaminase Apoptosis Cancer
    GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
    GLS1 Inhibitor-4
  • HY-145713A
    GS-8873 TFA

    HBV-IN-19 TFA

    		 HBV Infection
    GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
    GS-8873 TFA
  • HY-157840
    Anti-infective agent 9

    		Parasite Infection
    Anti-infective agent 9 (compound 1) is a Plasmodium falciparum inhibitor (IC50=600 nM), can downregulate pyruvate levels and TCA cycle in Plasmodium. Anti-infective agent 9It has good metabolic stability and low toxicity to human liver cells. The study found, Anti-infective agent 9Potential targets for inhibiting Plasmodium falciparum are not 1-deoxidation-d-xylulose-5-Phosphate synthase (DXPS) .
    Anti-infective agent 9
  • HY-115981
    NS5A-IN-2

    		HCV Protease Infection
    NS5A-IN-2 (Compound 33) is a potent inhibitor of NS5A. NS5A-IN-2 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability . NS5A-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NS5A-IN-2
  • HY-146302
    14-3-3η Protein inhibitor 1
    2 Publications Verification

    		 Apoptosis Cancer
    14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
    14-3-3η Protein inhibitor 1
  • HY-124623
    DNDI-8219

    		Parasite Infection
    DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
    DNDI-8219
  • HY-155061
    hCYP1B1-IN-1

    		Cytochrome P450 Aryl Hydrocarbon Receptor Cancer
    hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM)，as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
    hCYP1B1-IN-1
  • HY-156102
    c-ABL-IN-5

    		Bcr-Abl Neurological Disease
    c-ABL-IN-5 is a selective c-Abl inhibitor with neuroprotective effects. c-ABL-IN-5 has blood-brain barrier penetrability, metabolic stability and good pharmacokinetic properties. When c-ABL-IN-5 is labeled with [18F] (compound [18F]3), it can be used as a tracer to evaluate disease-modifying efficacy by complementary positron emission tomography (PET). c-ABL-IN-5 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
    c-ABL-IN-5
  • HY-162630
    HDAC6-IN-44

    		HDAC Inflammation/Immunology
    HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis .
    HDAC6-IN-44
  • HY-169064
    HIV-1 inhibitor-75

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor, with an EC50 value ranging from 0.0039 to 0.338 μM. The binding target of HIV-1 inhibitor-75 is reverse transcriptase, with an IC50 value of 0.055 μM. HIV-1 inhibitor-75 shows good in vitro metabolic stability, exhibiting moderate clearance rates and a longer half-life in human plasma and liver microsomes .
    HIV-1 inhibitor-75
  • HY-169119
    Antifungal agent 114

    		Cytochrome P450 Fungal Infection
    Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .
    Antifungal agent 114
  • HY-143880
    MRGPRX1 agonist 4

    		Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
    MRGPRX1 agonist 4
  • HY-168526
    Keap1-Nrf2-IN-24

    		Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-24 (compound 57) is a potent Keap1-Nrf2 inhibitor with a Ki value of 13 nM. Keap1-Nrf2-IN-24 increases the protein expression of TRXR1 and NQO1. Keap1-Nrf2-IN-24 increases the AKR1B10 mRNA expression. Keap1-Nrf2-IN-24 shows good metabolic stability .
    Keap1-Nrf2-IN-24
  • HY-163783
    CSNK2-IN-1

    		Casein Kinase Infection
    CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
    CSNK2-IN-1
  • HY-164477
    FL442

    		Androgen Receptor Cancer
    FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
    FL442
  • HY-115982
    NS5A-IN-3

    		HCV Protease Infection
    NS5A-IN-3 (Compound 15) is a potent inhibitor of NS5A. NS5A-IN-3 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability. NS5A-IN-3 exhibits a higher resistance barrier than daclatasvir against genotype 1b . NS5A-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NS5A-IN-3
  • HY-146201
    PDE4B/7A-IN-1

    		Phosphodiesterase (PDE) Others
    1 a /5-hydroxynitrile rubber 7 receptor antagonist (5-HT1 a k i = 8 nm, kb= 0.04 nm; 5-nitrile rubber 7K I = 451 nm, kb= 460 nm) has pde4b/pde7a inhibitory activity (PDE4B ic50= 80.4 μ M; Pde7a chip 50= 151.3 μ M）。 Compound 22 has a very good ability of passive penetration of biofilm and high metabolic stability in vitro. In addition, 22's pharmacological evaluation showed its pre cognitive and antidepressant properties in rat behavioral tests.
    PDE4B/7A-IN-1
  • HY-121081
    BAY-958

    		CDK Cancer
    BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
    BAY-958

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