122 Results for "

human microsomes

" in MedChemExpress (MCE) Product Catalog:
Products (122)

122 Results for "human microsomes" in MCE Product Catalog:

Cat. No.: HY-162409
CAS No.: 3057206-41-1
Research Areas:  

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 .
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Cat. No.: HY-162525
CAS No.: 2306328-43-6
Target:  

HIV Protease

Research Areas:  

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 .
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Cat. No.: HY-N7454
CAS No.: 23893-13-2
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
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Cat. No.: HY-10864R
CAS No.: 546141-08-6
Synonyms: KDS-4103 (Standard)
URB-597 (Standard) is the analytical standard of URB-597. This product is intended for research and analytical applications. 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 .
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Cat. No.: HY-146410
CAS No.: 2709031-17-2
Target:  

Angiotensin Receptor

Research Areas:  

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 .
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Cat. No.: HY-117428
CAS No.: 1513828-41-5
Target:  

11β-HSD

Research Areas:  

Metabolic Disease

INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .
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Cat. No.: HY-113777
CAS No.: 90780-46-4
Synonyms: 22-Hydroxy Docosahexaenoic acid; 22-OH DHA
Target:  

Cytochrome P450

Research Areas:  

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.
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Cat. No.: HY-112690
CAS No.: 625095-60-5
Target:  

Cytochrome P450

Research Areas:  

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.
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Cat. No.: HY-137580
CAS No.: 153525-55-4
Target:  

Cytochrome P450

Research Areas:  

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.
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Cat. No.: HY-N8094
CAS No.: 101236-51-5
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 .
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Cat. No.: HY-100644
CAS No.: 27653-68-5
Synonyms: Trimethoprim 1-N-oxide
Target:  

Drug Metabolite

Research Areas:  

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 .
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Cat. No.: HY-172093
Target:  

HIV

Research Areas:  

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 .
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Cat. No.: HY-113986B
CAS No.: 102676-86-8
Synonyms: (S)-Fadrozole; (S)-CGS 16949A free base; (S)-FAD286
(S)-Dexfadrostat ((S)-Fadrozole) is an aromatase inhibitor with an IC50 of 4.6 nM in human placental microsomes in vitro. (S)-Dexfadrostat can be used in the study of estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus .
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Cat. No.: HY-171278
CAS No.: 1095750-94-9
Target:  

Casein Kinase

Research Areas:  

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% .
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Cat. No.: HY-N11676
CAS No.: 1035154-49-4
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 .
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Cat. No.: HY-146111
CAS No.: 2667681-57-2
Target:  

IRAK

Research Areas:  

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 .
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Cat. No.: HY-N11827
CAS No.: 22672-74-8
Synonyms: (+)-Isocorybulbine
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 .
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Cat. No.: HY-139721
CAS No.: 2611373-80-7
Target:  

HIV

Research Areas:  

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.
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Cat. No.: HY-173426
Target:  

SARS-CoV

Research Areas:  

Infection

SARS-CoV-2 Mpro-IN-40 (compound 119) is an inhibitor of SARS-CoV-2 Mpro, with an IC50 value of 15.7 nM against Mpro Fret. SARS-CoV-2 Mpro-IN-40 exhibits low metabolic stability in human microsomes .
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Cat. No.: HY-151957
CAS No.: 2883173-23-5
Target:  

Bacterial

Research Areas:  

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 .
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