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human liver microsomes

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79

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11

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3

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N5132
    (-)-Fenchone

    		Others Others
    (-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .
    (-)-Fenchone
  • HY-112690A
    Pradefovir mesylate
    1 Publications Verification

    Remofovir mesylate

    		 Cytochrome P450 Metabolic Disease
    Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
    Pradefovir mesylate
  • HY-16718
    Dagrocorat

    PF-00251802

    		 Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
    Dagrocorat
  • HY-16718A
    Dagrocorat hydrochloride

    PF-00251802 hydrochloride

    		 Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
    Dagrocorat hydrochloride
  • HY-100644
    Trimethoprim N-oxide

    Trimethoprim 1-N-oxide

    		 Drug Metabolite Infection
    Trimethoprim N-oxide (Trimethoprim 1-N-oxide) belongs to human urinary metabolites. Trimethoprim N-oxide is generated by oxidation of nitrogen atoms in the pyrimidine ring. Trimethoprim N-oxide is formed predominantly by CYP1A2 in human liver microsomes .
    Trimethoprim N-oxide
  • HY-N8094
    Kushenol M

    		Cytochrome P450 Others
    Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
    Kushenol M
  • HY-N5132R
    (-)-Fenchone (Standard)

    		Others Others
    (-)-Fenchone (Standard) is the analytical standard of (-)-Fenchone. This product is intended for research and analytical applications. (-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .
    (-)-Fenchone (Standard)
  • 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-112690
    Pradefovir

    		Cytochrome P450 Metabolic Disease
    Pradefovir is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
    Pradefovir
  • HY-B0794S
    AZ7550-d5

    		EGFR IGF-1R Drug Metabolite Others
    AZ7550-d5 is the deuterium labeled AZ7550?(HY-B0794). AZ7550, an active metabolite of Osimtinib (AZD9291; HY-15772), inhibits the activity of?IGF1R?with an?IC50?of 1.6 μM .
    AZ7550-d5
  • HY-137580
    N-Desmethyl Eletriptan

    		Cytochrome P450 Metabolic Disease
    N-desmethyl Eletriptan is a metabolite of Eletriptan (HY-A0039). It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes.
    N-Desmethyl Eletriptan
  • 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-171185
    CP-611,781

    		Drug Metabolite Others
    CP-611,781 is a diol metabolite of ezlopitant alkene (CJ-12,458). In human liver microsomes, the apparent KM value of 5.4 μM for the formation of CP-611,781 .
    CP-611,781
  • HY-113777
    22-HDHA

    22-Hydroxy Docosahexaenoic acid; 22-OH DHA

    		 Cytochrome P450 Metabolic Disease
    22-HDHA (22-Hydroxy Docosahexaenoic acid) is an oxidation product of docosahexaenoic acid. In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
    22-HDHA
  • 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-117789
    Keto-itraconazole

    keto-ITZ

    		 Cytochrome P450 Infection Cancer
    Keto-itraconazole (keto-ITZ) is a metabolism of Itraconazole (HY-17514) with a potent inhibitor activity of CYP3A. Keto-itraconazole shows unbound IC50 value of 4.6 nM when coincubated with human liver microsomes and midazolam .
    Keto-itraconazole
  • HY-B0476
    Phenacetin

    Acetophenetidin

    		 COX Inflammation/Immunology
    Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin
  • HY-N1483
    Guanfu base A

    		Potassium Channel Cardiovascular Disease
    Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
    Guanfu base A
  • HY-N11677
    7-Hydroxy-TSU-68

    		Drug Metabolite Others
    7-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .
    7-Hydroxy-TSU-68
  • HY-139347
    Mazisotine

    		Somatostatin Receptor Neurological Disease Inflammation/Immunology
    SSTR4 agonist-1 (Compound 47) is a selective agonist for somatostatin receptor subtype 4 (SSTR4) with an EC50 of 4.7 nM. SSTR4 agonist-1 reveals a half-life > 130 minutes in human liver microsomes .
    Mazisotine
  • HY-N11676
    6-Hydroxy-TSU-68

    		Drug Metabolite Cancer
    6-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .
    6-Hydroxy-TSU-68
  • HY-171278
    Casein kinase 1δ-IN-28

    		Casein Kinase Metabolic Disease Cancer
    Casein kinase 1δ-IN-28 (Compound 4) is the inhibitor for CK1ε with an IC50 of 0.0146 μM. Casein kinase 1δ-IN-28 exhibits a metabolite rate in human liver microsomes of 52% .
    Casein kinase 1δ-IN-28
  • HY-129105
    Clomethiazole
    3 Publications Verification

    		 GABA Receptor Cytochrome P450 Neurological Disease
    Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
    Clomethiazole
  • HY-146111
    IRAK4-IN-13

    		IRAK Cancer
    IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg .
    IRAK4-IN-13
  • 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-139721
    Tenofovir-C3-O-C15-CF3 ammonium

    		HIV Infection
    Tenofovir-C3-O-C15-CF3 (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
    Tenofovir-C3-O-C15-CF3 ammonium
  • 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-151957
    Antitubercular agent 34

    		Bacterial Infection
    Antitubercular agent 34 (compound 42g) is an antitubercular agent. Antitubercular agent 34 inhibits the growth of MtbH37Rv with a MIC90 value of 1.25 μg/mL with the ability of escaping metabolic degradation by human liver microsomes. Antitubercular agent 34 can be used for the research of tuberculosis .
    Antitubercular agent 34
  • HY-B0476S
    Phenacetin-d5

    Acetophenetidin-d5

    		 COX Inflammation/Immunology
    Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin-d5
  • 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-B0476S1
    Phenacetin-13C

    		COX Inflammation/Immunology
    Phenacetin- 13C is the 13C labeled Phenacetin . Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin-13C
  • HY-171462
    SMW139

    		P2X Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    SMW139 is a selective allosteric antagonist of P2X7 receptor, with a Ki value of 32 nM for human P2X7R. The half-life of SMW139 in rat liver microsomes is 47 minutes. SMW139 can be used for inflammation, Alzheimer’s disease, multiple sclerosis study .
    SMW139
  • HY-157931
    Anticancer agent 192

    		Histamine Receptor Neurological Disease
    Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
    Anticancer agent 192
  • HY-17614
    Ezutromid

    SMT C1100; BMN 195; VOX-C1100

    		 Cytochrome P450 Others
    Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
    Ezutromid
  • 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-B0476R
    Phenacetin (Standard)

    Acetophenetidin (Standard)

    		 Reference Standards COX Inflammation/Immunology
    Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin (Standard)
  • HY-149481
    D4R agonist-1

    		Dopamine Receptor Neurological Disease
    D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders .
    D4R agonist-1
  • HY-10864
    URB-597
    5 Publications Verification

    KDS-4103

    		 FAAH Autophagy Mitophagy Neurological Disease
    URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
    URB-597
  • 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-162409
    PAR4 antagonist 4

    		Protease Activated Receptor (PAR) Others
    PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
    PAR4 antagonist 4
  • 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-143326
    Antibacterial agent 83

    		Bacterial Infection
    Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes .
    Antibacterial agent 83
  • HY-162408
    PAR4 antagonist 3

    		Protease Activated Receptor (PAR) Others
    PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
    PAR4 antagonist 3
  • HY-150508
    MK-0159

    		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-130431
    Vinclozolin M2

    		Parasite Infection
    Vinclozolin M2 is an active metabolite of vinclozolin. It is formed from vinclozolin by successive esterase activity and decarboxylation of vinclozolin in C. elegans and by decarboxylation in human liver microsomes. Vinclozolin M2 is an antagonist of the mineralocorticoid receptor (IC50=1,400 nM) and androgen receptor (IC50=0.17 nM) in reporter assays using MCF-7 cells.
    Vinclozolin M2
  • 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-162526
    HIV capsid modulator 2

    		HIV Infection
    HIV capsid modulator 2 (Compound 7t) is a modulator for the HIV capsid (CA) protein. HIV capsid modulator 2 exhibits antiviral activity, which inhibits HIV-1 IIIB strain and HIV-2 ROD strain with EC50 of 0.04 and 0.13 μM. HIV capsid modulator 2 is metabolically stable in human liver microsomes .
    HIV capsid modulator 2
  • 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-W424918
    Opromazine hydrochloride

    		Dopamine Receptor Neurological Disease
    Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.
    Opromazine hydrochloride
  • HY-162238
    OSM-S-106

    		Parasite Infection
    OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
    OSM-S-106

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