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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
77 Results for "
rat microsomes
" in MedChemExpress (MCE) Product Catalog:
Products (77)
77 Results for "rat microsomes" in MCE Product Catalog:
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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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3 Cited Publications
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17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes . 17-ODYA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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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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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 .
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1 Cited Publications
Cat. No.: HY-N3807
CAS No.: 19914-20-6
Category:
Cardiovascular Disease Infection Alkaloids Microorganisms Other Alkaloids Disease Research Fields
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1 Cited Publications
Cat. No.: HY-N4070
CAS No.: 73566-30-0
Category:
Flavonoids Glycine max (L.) merr Other Diseases Phenols Polyphenols Leguminosae Extract Plants Disease Research Fields Isoflavones
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1 Cited Publications
Cat. No.: HY-N4071
CAS No.: 71385-83-6
Category:
Flavonoids Monophenols Glycine max (L.) merr Other Diseases Phenols Leguminosae Extract Plants Disease Research Fields Isoflavones
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Cat. No.: HY-153508
CAS No.: 2098490-06-1
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ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
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 .
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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 .
Cat. No.: HY-N4031
CAS No.: 82375-29-9
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S-(p-Nitrobenzyl)glutathione is a competitive glutathionase inhibitor. S-(p-Nitrobenzyl)glutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-(p-Nitrobenzyl)glutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system .
Cat. No.: HY-128268
CAS No.: 735303-62-5
PFK-IN-1 (compound 1) is a phosphofructokinase (PFK) inhibitor, with IC50 values of 0.41 and 0.23 μM against T.brucei and T.cruzi PFK, respectively, and an ED50 of 15.18 μg/mL for T.brucei. The half-lives of PFK-IN-1 in rat and mouse liver microsomes are 9.7 and 408 minutes, respectively .
Cat. No.: HY-173084
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BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes .
Synonyms: DETC-Me; DDTC-Me; Diethyldithiocarbamic acid methyl ester
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S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) is the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram (HY-B0240). It is produced by the methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) inhibits rat liver low Km aldehyde dehydrogenase (ALDH) (ID50=15.5 mg/kg). When administered at a dose of 20.6 mg/kg, it decreases mean arterial pressure (MAP) and increases heart rate in rats during ethanol stimulation.
Synonyms: Glycyrrhetic acid 3-O-hydrogen sulfate
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18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC50 of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research .
Cat. No.: HY-W003371
CAS No.: 134521-16-7
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CGP 44 645 is the methanol metabolite of Letrozole (HY-14248) and is a molecular indicator for evaluating its metabolic kinetics in microsomes in vitro. Levels of CGP 44 645 in rat liver microsomes may be sex-specific .
Cat. No.: HY-W196803
CAS No.: 629-19-6
Synonyms: Propyl Disulfide; DPDS
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Dipropyl disulfide is oxidized to dipropyl thiosulfinate (DPDSO) by rat microsomes. Both flavincontaining monooxygenases (FMO) and cytochrome P450 enzymes (CYPs) are involved in dipropyl disulfide oxidation. Dipropyl disulfide forms two metabolites: propylglutathione sulfide conjugate and propylthiol .
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YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones .
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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
