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liver microsome stability

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100432
    LOC14
    4 Publications Verification

    		 PDI Neurological Disease Inflammation/Immunology
    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding . LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
    LOC14
  • HY-150508
    MK-0159
    1 Publications Verification

    		 CD38 Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
    MK-0159
  • HY-160023
    Elisrasib

    D3S-001

    		 Ras PERK Cancer
    Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. 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-157421
    Nampt activator-4

    		NAMPT Metabolic Disease
    Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
    Nampt activator-4
  • HY-15163
    Zotiraciclib
    2 Publications Verification

    TG02; SB1317

    		 JAK CDK FLT3 Cancer
    Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
    Zotiraciclib
  • HY-107460
    LDN-211904 oxalate
    1 Publications Verification

    		 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-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-146486
    P2Y2R/GPR17 antagonist 1

    		P2Y Receptor Inflammation/Immunology
    P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes .
    P2Y2R/GPR17 antagonist 1
  • HY-152118
    CYP1B1-IN-4

    		Cytochrome P450 Cancer
    CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
    CYP1B1-IN-4
  • HY-112388
    GSK-3b Inhibitor XI
    1 Publications Verification

    		 GSK-3 Neurological Disease Metabolic Disease
    GSK-3b Inhibitor XI (Compound 33) is a potent and selective GSK3β inhibitor, with a Ki value of 25 nM. GSK-3b Inhibitor XI increases glycogen synthase (GS) activity. GSK-3b Inhibitor XI can be used for research on type 2 diabetes and Alzheimer’s disease .
    GSK-3b Inhibitor XI
  • HY-163032
    FABP4-IN-3

    		FABP Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 Ki = 25 ± 3 a nM, FABP3 Ki = 15.03 μM) which exhibits a 601-fold selectivity over FABP3. FABP4-IN-3 also shows metabolic stability and potent cellular anti-inflammatory activity, making it promising to get involved in the research of metabolic disease, cardiac dysfunction and inflammation-related disease .
    FABP4-IN-3
  • HY-173084
    BRD6257

    		Phosphatase MDM-2/p53 Cancer
    BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes .
    BRD6257
  • HY-157325
    RIPK2-IN-5

    		RIP kinase Inflammation/Immunology
    RIPK2-IN-5 (compound 14) is a high affinity and excellent selectivity RIPK2 inhibitor with an IC50 value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases .
    RIPK2-IN-5
  • HY-175533
    TLR2 antagonist-1

    		Toll-like Receptor (TLR) Neurological Disease Inflammation/Immunology
    TLR2 antagonist-1 is a selective Toll-like receptor 2 (TLR2) antagonist. TLR2 antagonist-1 can effectively inhibit excessive TLR2 activation (IC50 = 11.41 μM) and the production of inflammatory factors. TLR2 antagonist-1 has metabolic stability with a half-life (T1/2) of 16.67 min in mouse liver microsomes. TLR2 antagonist-1 can be used for the researches of inflammation, immunology, and neurological disease .
    TLR2 antagonist-1
  • HY-143255
    Enpp-1-IN-11

    		Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
    Enpp-1-IN-11
  • HY-156672
    S6K2-IN-1

    		FGFR Cancer
    S6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC50: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC50: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes .
    S6K2-IN-1
  • 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-169402A
    PDE1-IN-9 hydrochloride

    		Phosphodiesterase (PDE) NO Synthase Reactive Oxygen Species (ROS) Interleukin Related Inflammation/Immunology
    PDE1-IN-9 (Compound 7a) hydrochloride is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 hydrochloride reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 hydrochloride exhibits good metabolic stability in rat liver microsomes .
    PDE1-IN-9 hydrochloride
  • HY-148060
    JAK-IN-21
    1 Publications Verification

    		 JAK Cancer
    JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively .
    JAK-IN-21
  • 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-149920
    Anticancer agent 98

    		Microtubule/Tubulin Cancer
    Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
    Anticancer agent 98
  • HY-155050
    PRMT5-IN-31

    		Apoptosis Histone Methyltransferase Cancer
    PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
    PRMT5-IN-31
  • 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-172147
    SSTR4 agonist 5

    		Somatostatin Receptor Neurological Disease
    SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
    SSTR4 agonist 5
  • 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-146410
    AT2R antagonist 1

    		Angiotensin Receptor Others
    AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
    AT2R antagonist 1
  • HY-150578
    Keap1-Nrf2-IN-12

    		Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-12 is a potent Keap1-Nrf2 inhibitor with an IC50 value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes .
    Keap1-Nrf2-IN-12
  • HY-163291
    AM4085

    		Bacterial Infection
    AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
    AM4085
  • HY-120608
    BMS-814580

    		MCHR1 (GPR24) Metabolic Disease
    BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities .
    BMS-814580
  • 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-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-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-173120
    HBV-IN-51

    		HBV Infection
    HBV-IN-51 (Compound 17e) is a potent HBV capsid assembly modulator. HBV-IN-51 exhibits remarkable anti-HBV activity with an EC50 of 0.033 μM in HepAD38 cells. HBV-IN-51 exhibits robust metabolic stability in plasma, and can be rapidly metabolized in human liver microsomes .
    HBV-IN-51
  • HY-156093
    TPH1-IN-1

    		Tryptophan Hydroxylase Metabolic Disease
    TPH1-IN-1 (compound 40) is a xanthine derivative and an inhibitor of tryptophan hydroxylase TPH1 (IC50: 110.1 nM). TPH1-IN-1 has good in vitro activity and liver microsome stability, and effectively inhibits adipocyte differentiation of T3-L1 cells .
    TPH1-IN-1
  • 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-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-168572
    MZ82

    		BCRP Cancer
    MZ82, Ko 143 (HY-10010) derivative, is a ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor with the IC50 of ~23 nM. MZ82 not only shows greatly improved metabolic stability over Ko 143 (HY-10010) in liver microsomes but also in mice, and is able to penetrate into the brain .
    MZ82
  • HY-161663
    Phosphodiesterase-IN-2

    		Phosphodiesterase (PDE) Cardiovascular Disease
    Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
    Phosphodiesterase-IN-2
  • HY-40156A
    Mycobacterium Tuberculosis-IN-5

    		Bacterial Infection
    Mycobacterium Tuberculosis-IN-5 (Compound 11) is the HCl salt form of 5-Fluoroindole (HY-40156). Mycobacterium Tuberculosis-IN-5 is an antibacterial agent, that inhibits Mycobacterium tuberculosis with a MIC of 29.1 μM. Mycobacterium Tuberculosis-IN-5 exhibits metabolic stability in rat liver microsomes. Mycobacterium Tuberculosis-IN-5 exhibits anti-tuberculosis efficacy in mice .
    Mycobacterium Tuberculosis-IN-5
  • HY-149395
    MmpL3-IN-3

    		Bacterial Infection
    MmpL3-IN-3 (Compound 12) is a MmpL3 inhibitor. MmpL3-IN-3 shows a MIC of 0.1 μM against H37Rv. MmpL3-IN-3 shows good stability in mouse liver microsomes. MmpL3-IN-3 can be used for anti-tubercular research .
    MmpL3-IN-3
  • 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 Ovalbumin, low endotoxin (HY-W250978A)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
    BTL-MK
  • HY-168562
    σ1 Receptor ligand 1

    		Sigma Receptor Neurological Disease Cancer
    σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
    σ1 Receptor ligand 1
  • 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-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-169402
    PDE1-IN-9

    		Phosphodiesterase (PDE) NO Synthase Reactive Oxygen Species (ROS) Interleukin Related Inflammation/Immunology
    PDE1-IN-9 (Compound 7a) is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 exhibits good metabolic stability in rat liver microsomes .
    PDE1-IN-9
  • 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-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-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-168998
    Yck2-IN-1

    		Fungal Casein Kinase Infection
    Yck2-IN-1 (Compound 2a) is an inhibitor of the fungal Candida albicans Yck2 kinase. It exhibits an IC50 of approximately 80 nM against Yck2 and a MIC80 of 12.5 µM against C. albicans, with good metabolic stability (66% remaining in mouse liver microsomes). In a mouse model of drug-resistant candidiasis, Yck2-IN-1 significantly reduced fungal burden in the kidneys. Yck2-IN-1 holds promise for research in the field of antifungal infection .
    Yck2-IN-1
  • HY-162620
    α2A-AR agonist 1

    		Adrenergic Receptor Cancer
    α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
    α2A-AR agonist 1

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