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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
122 Results for "
human microsomes
" in MedChemExpress (MCE) Product Catalog:
Products (122)
122 Results for "human microsomes" in MCE Product Catalog:
Cat. No.: HY-168728
CAS No.: 894280-02-5
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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 .
Cat. No.: HY-150578
CAS No.: 2250082-04-1
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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 .
Cat. No.: HY-157931
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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 .
Cat. No.: HY-171462
CAS No.: 2133010-38-3
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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 .
Cat. No.: HY-149481
CAS No.: 2826198-44-9
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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 .
Cat. No.: HY-173120
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 .
Cat. No.: HY-129105R
CAS No.: 533-45-9
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Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. 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 .
Cat. No.: HY-162408
CAS No.: 3057206-40-0
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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 .
Cat. No.: HY-170486
CAS No.: 3104123-06-7
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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 .
Cat. No.: HY-130431
CAS No.: 83792-61-4
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.
Cat. No.: HY-123639
CAS No.: 261766-32-9
Synonyms: N-(2-Phenylethyl)-indomethacin amide
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LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
Cat. No.: HY-162787
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Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
Cat. No.: HY-162526
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 .
Cat. No.: HY-W424918
CAS No.: 316-07-4
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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.
Cat. No.: HY-151958
Antitubercular agent-35 (compound 42l) is an antitubercular agent. Antitubercular agent-35 inhibits the growth of MtbH37Rv and M. Marinum with MIC90 values of 1.25 and 2 μg/mL, respectively. Antitubercular agent-35 shows the ability of escaping metabolic degradation by human liver microsomes. Antitubercular agent-35 can be used for the research of tuberculosis .
Cat. No.: HY-169064
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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 .
Cat. No.: HY-125505
CAS No.: 1622159-00-5
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BI-11634 is an orally active factor Xa inhibitor and a CYP3A4 substrate. The apparent Km values for BI-11634 metabolism are 23 μM in human liver microsomes (HLMs) and 7.6 μM with recombinant CYP3A4. BI-11634 can be used for thromboembolic disease and CYP3A4-mediated drug metabolism research .
Cat. No.: HY-147754
CAS No.: 2243136-03-8
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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 .
Cat. No.: HY-17614R
CAS No.: 945531-77-1
Synonyms: SMT C1100 (Standard); BMN 195 (Standard); VOX-C1100 (Standard)
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Ezutromid (Standard) is the analytical standard of Ezutromid. This product is intended for research and analytical applications. 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 .
Cat. No.: HY-W707708
CAS No.: 60902-27-4
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
