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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
212 Results for "
microsomal
" in MedChemExpress (MCE) Product Catalog:
Products (212)
212 Results for "microsomal" in MCE Product Catalog:
Cat. No.: HY-P7899
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: ANPEP; LAP1; Prev. CD13; Myeloid Plasma Membrane Glycoprotein CD13; Prev. PEPN; Alanyl (Membrane) Aminopeptidase; Aminopeptidase N; Membrane Alanyl Aminopeptidase; Gp150; AP-M; AP-N; APN; HAPN; Alanyl Aminopeptidase; microsomal Aminopeptidase; CD13 Antige
Species:
Human
Source:
HEK293
Target:
Carboxylesterase (CES) Free Fatty Acid Receptor Reactive Oxygen Species (ROS) Mitochondrial Metabolism Ferroptosis Apoptosis
Research Areas:
GR148672X is an inhibitor of carboxylesterase 1 (CES1) and hepatic microsomal triglyceride hydrolase (TGH). GR148672X blocks the catalytic activity of CES1, impairs the functions of triglyceride and cholesteryl ester lipase, reduces triglyceride mobilization and secretion, and decreases apolipoprotein B-100 secretion in primary rat hepatocytes. Under low-glucose conditions, GR148672X inhibits the survival of colorectal cancer cells by reducing free fatty acid availability, inducing toxic triglyceride accumulation, ROS production, mitochondrial damage, ferroptosis and apoptosis. GR148672X can be used in studies related to colorectal cancer and atherosclerosis .
Cat. No.: HY-149916
CAS No.: 2922920-71-4
Target:
Research Areas:
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
Cat. No.: HY-184880
CAS No.: 1410114-25-8
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BMS-986144 non-deuterated is the non-tritium form of BMS-986144 (HY-131905S). BMS-986144 is an orally active inhibitor of HCV NS3/4A protease. BMS-986144 binds to the active site of HCV NS3/4A protease and induces conformational changes in the protease. BMS-986144 reduces time-dependent CYP3A4 inhibition, exhibits hepatic microsomal metabolic stability, and undergoes oxidation of the macrocyclic linker chain. BMS-986144 can be used in studies related to hepatitis C virus infection .
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Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
Cat. No.: HY-N19800
CAS No.: 1231899-06-1
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Target:
Cat. No.: HY-P11358
CAS No.: 159718-10-2
Research Areas:
Target:
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Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain .
Cat. No.: HY-121407A
CAS No.: 2180287-51-6
Target:
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(Rac)-Lateritin is an acyl-CoA:cholesterol acyltransferase (ACAT/SOAT) inhibitor, with IC50 values of 5.7 μM and 5.6 μM in rat liver, respectively. (Rac)-Lateritin exerts time-dependent irreversible enzyme inhibition that persists even after microsomal washing. (Rac)-Lateritin inhibits cholesterol ester formation in macrophages without altering triglyceride synthesis or other steps in oxidized low-density lipoprotein metabolism. (Rac)-Lateritin inhibits the growth of cancer cells, Gram-positive bacteria, and Candida albicans. (Rac)-Lateritin can be used in studies related to atherosclerosis, human solid tumors, mouse lymphocytic leukemia, as well as fungal and bacterial infections .
Cat. No.: HY-123882
CAS No.: 1604034-78-7
Target:
Research Areas:
IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
Cat. No.: HY-163982
Research Areas:
FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
Target:
Research Areas:
Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
Cat. No.: HY-117068S
Synonyms: (R,E)-Bromoenol lactone-d7
Research Areas:
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is the deuterated-labeled (R)-Bromoenol lactone (HY-117068). (R)-Bromoenol lactone ((R,E)-Bromoenol lactone) is an isomer of Bromoenol lactone (HY-107411). (R)-Bromoenol lactone acts as a selective inhibitor of microsomal calcium-independent phospholipase A2γ (iPLA2γ). (R)-Bromoenol lactone induces mild activation of p38 mitogen-activated protein kinase in prostate cancer cells, resulting in slight increases in the expressions of phosphorylated p53, total p53 and p21. (R)-Bromoenol lactone is applicable to prostate cancer-related research .
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Research Areas:
Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
Cat. No.: HY-182042
Target:
Research Areas:
DENV-IN-15 is a sulfonyl anthranilic acid derivative and a pan-serotype anti-dengue virus (DENV) inhibitor with broad-spectrum anti-RNA virus activity. The EC50 value of DENV-IN-15 against DENV-2 in Huh-7 cells is 0.7 μM. DENV-IN-15 selectively regulates the translation of mRNAs encoding translation-related proteins and containing a 5'-oligopyrimidine tract. DENV-IN-15 reduces the expression of specific ribosomal proteins, thereby inhibiting viral replication. DENV-IN-15 exhibits enhanced membrane permeability, human plasma stability and human liver microsomal metabolic stability. DENV-IN-15 is applicable to research related to dengue virus infection .
Cat. No.: HY-182244
Target:
Research Areas:
SERT/NET-IN-1 is a blood-brain barrier-permeable SERT and NET inhibitor, with an IC50 of 11.2 nM against human SERT and an IC50 of 32.0 nM against human NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET-IN-1 can be used in studies related to premature ejaculation .
Cat. No.: HY-A0069AS
CAS No.: 1173020-59-1
Category:
Other Monoterpenes Umbelliferae Extract Terpenoids Other Diseases Plants Vernonia Schreb. Disease Research Fields
Target:
Cat. No.: HY-W331198
CAS No.: 122454-29-9
Target:
Research Areas:
Tralopyril is an orally active, blood-brain barrier-penetrating antifouling insecticide and endocrine disruptor. By interfering with the thyroid hormone system and mitochondrial oxidative phosphorylation, Tralopyril downregulates the transcription of genes such as TRHR, Nkx2.1, TRα and induces ferroptosis. Tralopyril disrupts amino acid, energy and lipid metabolism, exhibits significant skeletal and reproductive toxicity, and causes developmental damage. Tralopyril has a long half-life in vivo and wide tissue distribution, posing potential risks to aquatic organisms and human health. Tralopyril shows species specificity in in vitro liver microsomal metabolism, exerts lethal effects on target insects and laboratory animals, and is commonly used in studies of chlorfenapyr poisoning and related toxic mechanisms .
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Research Areas:
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) . YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research .
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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
