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Pathways Recommended: Metabolic Enzyme/Protease
Results for "

good metabolic stability

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75

Inhibitors & Agonists

1

Screening Libraries

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

    		Aminoacyl-tRNA Synthetase 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-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-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-170571
    BE2647

    		Mitochondrial Metabolism Metabolic Disease Inflammation/Immunology
    BE2647 is a selective inhibitor for mitochondrial pyruvate carrier (MPC) with an EC50 of 70 nM. BE2647 exhibits good metabolic stability in mouse liver microsomes. BE2647 can be used in research of metabolic diseases, non-alcoholic fatty liver disease (MASLD), or non-alcoholic steatohepatitis (MASH) .
    BE2647
  • HY-168728
    MAO-B-IN-37

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-37 (Compound 37) is a derivative of TT01001 (HY-114520), and a selective inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 270 nM. MAO-B-IN-37 exhibits good metabolic stability in mice microsomes and good affinity with human serum albumin .
    MAO-B-IN-37
  • HY-172423
    Darlifarnib

    		Farnesyl Transferase Cancer
    Darlifarnib (Compound (S)-058) is the inhibitor for farnesyl transferase and geranylgeranyltransferase with IC50 ≤ 10 nM and ＞ 1000 nM. Darlifarnib exhibits good metabolic stability in human and mouse liver microsomes with the half-life time ＞ 100 min .
    Darlifarnib
  • 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-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-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-170546
    MU1920

    		Haspin Kinase Cancer
    MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes .
    MU1920
  • HY-172093
    HIV-1 inhibitor-80

    		HIV Infection
    HIV-1 inhibitor-80 (compound M44) is an HIV-1 inhibitor with an EC50 of 5-148 nM. HIV-1 inhibitor-80 shows good metabolic stability and cytotoxicity in human plasma and human liver microsomes .
    HIV-1 inhibitor-80
  • HY-162928
    RIPK1-IN-26

    		RIP kinase 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-160023
    Elisrasib

    D3S-001

    		 Ras Cancer
    Elisrasib is an orally active inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. Elisrasib 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 .
    Elisrasib
  • 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-174454
    Antitrypanosomal agent 24

    		P-glycoprotein Infection
    Antitrypanosomal agent 24 is a benzothiazole amidoxime with strong and selective antitrypanosomal activity (IC50 = 0.92 μM). Antitrypanosomal agent 24 is a substrate of the P-glycoprotein efflux pump. Antitrypanosomal agent 24 has high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA by intercalation .
    Antitrypanosomal agent 24
  • 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-170945
    Antidepressant agent 9

    		iGluR Serotonin Transporter Neurological Disease
    Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test .
    Antidepressant agent 9
  • 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-170486
    MLK3-IN-1

    		Mixed Lineage Kinase FAK Cancer
    MLK3-IN-1 (Compound 37) is a selective inhibitor for mixed-lineage protein kinase 3 (MLK3) with an IC50 <1 nM. MLK3-IN-1 inhibits FAK with an IC50 of 15.5 μM. MLK3-IN-1 exhibits good metabolic stability in mouse and human liver microsomes .
    MLK3-IN-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-155538
    Cisd2 agonist 1

    		Mitophagy 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-158316
    BTL-MK

    		Fc Receptor (FcR) 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-169927
    Ferroptosis-IN-16

    		Ferroptosis Inflammation/Immunology
    Ferroptosis-IN-16 (Compound 13l) is a specific inhibitor for ferroptosis with an EC50 of 0.7 nM and 0.9 nM in ES-2 cell and LX-2 cell. Ferroptosis-IN-16 ameliorates Acetaminophen (HY-66005)-induced acute liver injury in mouse model, and exhibits good metabolic stability in mouse liver microsomes .
    Ferroptosis-IN-16
  • HY-136358
    LDN-211904

    		Ephrin Receptor Cancer
    LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC .
    LDN-211904
  • 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-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-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-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-144898
    SB-216

    		Microtubule/Tubulin Apoptosis Cancer
    SB-216 is an BBB-penetrable tubulin polymerization inhibitor. SB-216 can inhibit the proliferation and migration, and induce apoptosis and cell cycle arrest of tumor cells. SB-216 has good in vivo metabolic stability and low toxicity, but its oral bioavailability is limited. SB-216 has antitumor activity and can be used in the research of tumors such as melanoma .
    SB-216
  • HY-107460
    LDN-211904 oxalate

    		Ephrin Receptor Cancer
    LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
    LDN-211904 oxalate
  • HY-174348
    BRD4-IN-10

    		Epigenetic Reader Domain Inflammation/Immunology
    BRD4-IN-10 (Compound 31) is a selective BRD4 inhibitor with an IC50 of 13.5 nM. BRD4-IN-10 can exert anti-inflammatory and anti-fibrotic effects. BRD4-IN-10 also has good metabolic stability, pharmacokinetic properties and safety. BRD4-IN-10 can be used in the research of renal fibrosis diseases .
    BRD4-IN-10
  • 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-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-153508
    ANO1-IN-4

    		Chloride Channel Others
    ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
    ANO1-IN-4
  • 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-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-163763
    T-10418

    		G2A (GPR132) Neurological Disease Inflammation/Immunology Cancer
    T-10418 is a potent and highly selective G2A/GPR132 agonist. T-10418 has an EC50 of 0.82 μM for human G2A activation. T-10418 has good water solubility, metabolic stability, and pharmacokinetic properties. T-10418 can be used for the research of various diseases such as neuropathic pain, acute myeloid leukemia, and inflammation .
    T-10418
  • HY-168956
    Pks13-IN-2

    		Bacterial Infection
    Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 shows good metabolic stability in mouse liver microsomes and hepatocytes. Pks13-IN-2 can be used for tuberculosis research .
    Pks13-IN-2
  • 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-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

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