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human microsomes

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238

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0476
    Phenacetin
    1 Publications Verification

    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-N0904
    Ginsenoside C-K
    5 Publications Verification

    Ginsenoside compound K; Ginsenoside K

    		 COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Ginsenoside C-K
  • 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-129105
    Clomethiazole
    4 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-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-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-W010981
    Acetyl tributyl citrate
    1 Publications Verification

    Tributyl O-acetylcitrate; ATBC

    		 Environmental Pollutants Biochemical Assay Reagents Others
    Acetyl tributyl citrate (Tributyl O-acetylcitrate) is a pharmaceutical excipient and biodegradable hydrophobic plasticizer. Acetyl tributyl citrate can be used in cosmetics, food packaging, and as a flavoring substance for food .
    Acetyl tributyl citrate
  • HY-125643
    Pitavastatin lactone

    		Drug Metabolite Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Pitavastatin lactone is a major metabolite of Pitavastatin (HY-B0144A) in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase .
    Pitavastatin lactone
  • 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-120868
    TP-004
    1 Publications Verification

    		 MetAP Metabolic Disease Cancer
    TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM against MetAP2. TP-004 is a chemical probe. TP-004 suppresses MetAP2 enzymatic activity, blocks N-terminal methionine cleavage, impairs protein maturation and stability, and thereby inhibits cell proliferation and angiogenesis. TP-004 can be used for the study of tumors and diseases associated with excessive angiogenesis .
    TP-004
  • HY-A0296
    Chlormethiazole hydrochloride
    4 Publications Verification

    Clomethiazole hydrochloride

    		 Cytochrome P450 Neurological Disease
    Clomethiazole hydrochloride is a potent and orally active GABAA agonist . Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
    Chlormethiazole hydrochloride
  • HY-117290
    BMS-962212

    		Factor Xa Cardiovascular Disease
    BMS-962212 is a factor XIa (FXIa) inhibitor with a Ki of 0.7 nM against human FXIa and a Ki of 3 nM against rabbit FXIa. BMS-962212 blocks thrombosis while preserving normal hemostatic function. BMS-962212 is applicable to thrombosis-related research .
    BMS-962212
  • HY-N6745
    Citreoviridin

    		Na+/K+ ATPase Apoptosis Infection Cardiovascular Disease
    Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
    Citreoviridin
  • HY-142686A
    SGK1-IN-3 hydrochloride

    		SGK CDK P-glycoprotein Inflammation/Immunology
    SGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis .
    SGK1-IN-3 hydrochloride
  • HY-N4031
    Humantenine

    		Anaplastic lymphoma kinase (ALK) METTL3 Inflammation/Immunology
    Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes .
    Humantenine
  • 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-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-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-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-B0476R
    Phenacetin (Standard)
    1 Publications Verification

    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-19121A
    TCV-309 chloride

    		Platelet-activating Factor Receptor (PAFR) Cancer
    TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock .
    TCV-309 chloride
  • 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-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-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-148075
    PI4KIIIbeta-IN-11

    		PI4K Infection
    PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ, with a mean pIC50 value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum .
    PI4KIIIbeta-IN-11
  • HY-175045
    77PD-Q

    		Bacterial Infection
    77PD-Q is a p-phenylenediamine (PPD) derivative. 77PD-Q exhibits toxic to the aquatic bacterium V. fischeri. 77PD-Q can be used as an exposure biomarker in environmental monitoring .
    77PD-Q
  • 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
  • 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-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-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-148868A
    Akt1&PKA-IN-2

    		Akt CDK Cancer
    Akt1&PKA-IN-2 (Compound R-29) is a AKT1 and PKA inhibitor with selectivity for CDK2, with IC50 values of 0.007 and 0.01 μM, respectively. Akt1&PKA-IN-2 is applicable for cancer research .
    Akt1&PKA-IN-2
  • 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-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-N13388
    5-Hydroxytryptophol-O-glucuronide

    UGT1A6

    		 Biochemical Assay Reagents Others
    5-Hydroxytryptophol-O-glucuronide is an authentic glucuronide standard and probe metabolite. 5-Hydroxytryptophol-O-glucuronide is used to detect the activity of human UGT1A6 in in vitro systems including human liver microsomes and recombinant UGT1A6 .
    5-Hydroxytryptophol-O-glucuronide
  • 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-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-172565
    Posaconazole D-glucuronide

    SCH 56592 D-glucuronide

    		 Drug Metabolite UGT Infection
    Posaconazole D-glucuronide (SCH 56592 D-glucuronide) is a glucuronide metabolite of the antifungal agent Posaconazole (HY-17373). Posaconazole D-glucuronide can be formed in human liver microsomes catalyzed by UGT1A4 .
    Posaconazole D-glucuronide
  • HY-P10331
    KSL 128114

    		SDCBP Cancer
    KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
    KSL 128114
  • 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-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-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-162525
    GS-9770

    		HIV Protease Infection
    GS-9770 is an orally active inhibitor for HIV protease with Ki of 0.16 nM. GS-9770 exhibits antiviral activity aginst HIV-1 strains and HIV-2 strains with EC50 of 1.9-26 nM, and 26 nM. GS-9770 is metabolic stable in human liver microsomes. GS-9770 exhibits good pharmacokinetic characters in Sprague Dawley rats .
    GS-9770
  • 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-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-N5132R
    (-)-Fenchone (Standard)

    		Reference Standards 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-N11827
    Isocorybulbine

    (+)-Isocorybulbine

    		 Drug Metabolite Inflammation/Immunology
    Isocorybulbine ((+)-Isocorybulbine) is one of the main metabolites of Corydaline (HY-N0923) in human liver microsomes and liver cells. Corydaline has anti-acetylcholinesterase, anti-allergic, anti-allergic reaction and gastric emptying activities. Isocorybulbine can be used for the metabolic study of Corydaline .
    Isocorybulbine
  • 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-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-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

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