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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
198 Results for "
Liver microsomes
" in MedChemExpress (MCE) Product Catalog:
Products (198)
198 Results for "Liver microsomes" in MCE Product Catalog:
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5 Cited Publications
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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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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 .
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5 Cited Publications
Cat. No.: HY-N0904
CAS No.: 39262-14-1
Synonyms: Ginsenoside compound K; Ginsenoside K
Category:
Triterpenes Plant Terpenoids Panax ginseng C. A. Meyer Extract Disease Research Fields Inflammation/Immunology Araliaceae Extract
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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 .
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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 .
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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 .
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2 Cited Publications
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Mal-PEG4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker Mal-PEG4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682 .
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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 .
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1 Cited Publications
Cat. No.: HY-N4070
CAS No.: 73566-30-0
Category:
Leguminosae/Fabaceae Extract Plant Flavonoids Glycine max (L.) merr Extract Other Diseases Phenols Polyphenols Disease Research Fields Isoflavones
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1 Cited Publications
Cat. No.: HY-N4071
CAS No.: 71385-83-6
Category:
Leguminosae/Fabaceae Extract Plant Flavonoids Monophenols Glycine max (L.) merr Extract Other Diseases Phenols Disease Research Fields Isoflavones
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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.
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1 Cited Publications
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LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
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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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1 Cited Publications
Cat. No.: HY-N3807
CAS No.: 19914-20-6
Category:
Cardiovascular Disease Infection Alkaloids Other Alkaloids Microorganism Disease Research Fields
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Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
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 .
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 .
Cat. No.: HY-W130074
CAS No.: 1686-14-2
α-Pinene oxide is a type of monoterpene epoxidation intermediate. α-Pinene oxide is produced via the cytochrome P-450-mediated oxidation pathway in Dendroctonus terebrans body microsomes and rat liver microsomes, and can be further converted into alcohols, ketones and insect pheromone derivatives. α-Pinene oxide can generate the perfume intermediate myrtenal. α-Pinene oxide is used in studies related to terpenoid metabolism and perfume synthesis .
Cat. No.: HY-N4031
CAS No.: 82375-29-9
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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 .
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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
