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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
292 Results for "
human liver microsome
" in MedChemExpress (MCE) Product Catalog:
Products (292)
292 Results for "human liver microsome" in MCE Product Catalog:
6
6 Publications Verification
Synonyms: GDC-9545; RG6171
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Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER + breast cancer .
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5 Cited Publications
Cat. No.: HY-N0904
CAS No.: 39262-14-1
Synonyms: Ginsenoside compound K; Ginsenoside K
Category:
Panax ginseng C. A. Meyer Triterpenes Terpenoids Plants Disease Research Fields Inflammation/Immunology Araliaceae
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5
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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 .
4
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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 .
4
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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 .
2
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 .
2
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other families Flavonoids Monophenols Flavones Phenols Plants Disease Research Fields Cancer
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2
2 Cited Publications
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KDM4C-IN-1 is a histone lysine demethylase KDM4C inhibitor with an IC50 of 8 nM. KDM4C-IN-1 inhibits cancer cell proliferation. KDM4C-IN-1 can be used in the research of hepatocellular carcinoma and adenocarcinoma alveolar basal epithelial carcinoma .
1
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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 .
1
1 Cited Publications
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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 .
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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 .
1
1 Cited Publications
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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 .
1
1 Cited Publications
Synonyms: Remofovir mesylate
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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.
1
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Cardiovascular Disease Alkaloids other families Metabolic Disease Nelumbo nucifera Gaertn. Plants Disease Research Fields Isoquinoline Alkaloids Nymphaeaceae
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1
1 Cited Publications
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4-Hydroxyretinoic acid (4-HRA) is a derivative of Retinoic acid (HY-14649). 4-Hydroxyretinoic acid is formed via the catalysis of retinol by cytochrome P-450 isoenzymes. 4-Hydroxyretinoic acid also serves as a substrate for UDP-glucuronosyltransferase (s) and recombinant UGT2B7. 4-Hydroxyretinoic acid binds to the nuclear receptor RAR (Retinoic Acid Receptor), activates RAR and RXR-alpha, subsequently regulates gene expression and cell differentiation, and induces cancer cell apoptosis (Apoptosis). 4-Hydroxyretinoic acid also participates in multiple physiological processes such as immunoregulation, neuroprotection and antioxidation .
Cat. No.: HY-157421
CAS No.: 2847156-05-0
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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 .
Cat. No.: HY-17614
CAS No.: 945531-77-1
Synonyms: SMT C1100; BMN 195; VOX-C1100
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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 .
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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 .
Cat. No.: HY-N4031
CAS No.: 82375-29-9
Cat. No.: HY-16718
CAS No.: 1044535-52-5
Synonyms: PF-00251802
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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 .
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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
