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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
262 Results for "
microsome
" in MedChemExpress (MCE) Product Catalog:
Products (262)
262 Results for "microsome" in MCE Product Catalog:
Cat. No.: HY-182604
CAS No.: 1353712-58-9
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QC-308 is a HO-1/HO-2 inhibitor, with an IC50 of 0.27 μM against rat HO-1 and an IC50 of 0.46 μM against rat HO-2. QC-308 inhibits the activities of rat HO-1 and HO-2 in carbon monoxide generation assays using spleen and brain microsomes, respectively. QC-308 also exhibits senolytic activity, reducing the survival rate of adipogenic progenitor cells in skeletal muscle fibers of senescent mice and human skeletal muscle myoblasts. QC-308 is applicable for senescence-related research .
Cat. No.: HY-101016R
CAS No.: 34450-18-5
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17-ODYA (Standard) is the analytical standard of 17-ODYA. This product is intended for research and analytical applications. 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[1][2][3]. 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.
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-W275882
CAS No.: 13179-98-1
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1,6-Dimethoxyhexane is an aliphatic ether that serves as a PROTAC linker and fuel additive. 1,6-Dimethoxyhexane is an orally active testicular toxicant. It has no direct toxicity on its own, but exerts toxicity after oxidative metabolism by liver/testicular microsomes to produce 2-Methoxyacetic Acid (MAA). 1,6-Dimethoxyhexane induces apoptosis/necrosis of pachytene spermatocytes, downregulates the expression of HSP70.2, HSP60 and ERp60/PDI A3, and causes spermatogenic tubule degeneration, testicular/thymic atrophy, a sharp decline in epididymal sperm density, and other effects. 1,6-Dimethoxyhexane can be used in studies related to testicular toxicity .
Cat. No.: HY-142117
CAS No.: 149091-92-9
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Adenophostin A is an IP3 receptor (inositol 1,4,5-trisphosphate receptors) modulator and Ca 2+ releaser, with an IC50 of 1.3 nM, an EC50 of 1.4 nM, and a Ki of 0.18 nM in rats, and an IC50 of 0.95 nM in humans. Adenophostin A activates IP3 receptors, stimulates Ca 2+ release from intracellular stores and microsomes, inhibits the binding of [ 3H]IP3 to plasma membrane receptors, and activates chloride channels. Adenophostin A resists phosphorylation and dephosphorylation by IP3 metabolic enzymes to maintain its activity, and increases cytoplasmic [Ca 2+] levels via calcium mobilization from the endoplasmic reticulum of vascular smooth muscle cells. Adenophostin A is applicable to research related to hemorrhagic shock .
Cat. No.: HY-164111
CAS No.: 1128096-58-1
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JNK-IN-17 (Compound 9J) is a selective and potent JNK inhibitor with IC50 values of 0.039, 0.079 μM for JNK1 and JNK3. JNK-IN-17 can inhibit c-Jun phosphorylation with an IC50 of 0.082 μM in Streptozotocin (HY-13753)-infuced INS-1 pancreatic islet β cells. JNK-IN-17 shows inhibition rate ≤ 33% on the four main P450 subtypes (2C9, 2D6, 3A4, 1A2) in human liver microsomes, indicating a relatively low risk of drug interactions. JNK-IN-17 can be used for researches of neurological and metabolic disease, such as Parkinson's disease .
Cat. No.: HY-168251
CAS No.: 2933125-05-2
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PROTAC BRM/BRG1 degrader-3 is a BRM/BRG1 PROTAC degrader, exhibiting a DC50 of less than 1 nM for BRM degradation and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 shows moderate inhibitory activity against CYP2D6 and hERG. PROTAC BRM/BRG1 degrader-3 inhibits cancer cell proliferation and tumor tissue growth, and exhibits favorable metabolic stability in liver microsomes. PROTAC BRM/BRG1 degrader-3 can be used in non-small cell lung cancer-related research .
Cat. No.: HY-181710
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
Cat. No.: HY-181917
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Pantothenate kinase-IN-3 is an orally active PANK3-selective binder and CoA biosynthesis activator with a human PANK3 Ki of 9.1 nM, human PANK3 Ka of 1.8 nM, human PANK1β Ki of 113 nM, human PANK1β Ka of 23.4 nM, and oral effectiveness.Pantothenate kinase-IN-3 binds PANK3 via a water-mediated interaction between its sulfonamide NH and Gly193, elevates cellular, hepatic, and forebrain CoA levels, and shows improved metabolic stability in mouse and human microsomes.Pantothenate kinase-IN-3 has solubility properties favorable at pH 7.Pantothenate kinase-IN-3 can be used for the research of hepatic metabolic CoA deficiencies (acidemias) .
Synonyms: Glyoxaline (Standard); 1,3-Diaza-2,4-cyclopentadiene (Standard)
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Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
Cat. No.: HY-W016589
CAS No.: 1879-09-0
Synonyms: 6-tert-Butyl-2,4-xylenol
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2-(tert-Butyl)-4,6-dimethylphenol (6-tert-Butyl-2,4-xylenol) is an electrophilic alkylating agent, gasoline antioxidant and hydration substrate. 2-(tert-Butyl)-4,6-dimethylphenol inhibits SERCA activity in rabbit hindleg microsomes with an IC50 of 53 μM. Oxidation of 2-(tert-Butyl)-4,6-dimethylphenol generates the intermediate BDMP-QM, which covalently modifies nitrogen sites of proteins, polypeptides and free amino acids via Michael addition, triggering covalent modification of macromolecules and mediating cytotoxicity. 2-(tert-Butyl)-4,6-dimethylphenol is widely used in toxicological and biochemical studies of alkylphenols .
Cat. No.: HY-W699983
CAS No.: 74362-46-2
Synonyms: Glyoxaline-15N2; 1,3-Diaza-2,4-cyclopentadiene-15N2
Cat. No.: HY-181107
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DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC50 values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC50 of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia .
Cat. No.: HY-187120
CAS No.: 1422528-30-0
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PAIB-SOs-12 is a CYP1A1-activated antimitotic prodrug with affinity for human CYP1A1, with a Ki value of 1.2 μM. PAIB-SOs-12 exhibits nanomolar antiproliferative activity in cancer cells expressing CYP1A1, with a selectivity ratio of over 100 against cancer cells that do not express CYP1A1. PAIB-SOs-12 undergoes CYP1A1-mediated N-dealkylation to form the active metabolite PIB-SO, which induces G2/M cell cycle arrest and microtubule disruption, and shows significantly improved stability in rodent liver microsomes compared to its n-butyl analog. PAIB-SOs-12 can be used in breast cancer-related research .
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(3β)-3-(Acetyloxy)pregna-5,16-dien-20-one 20-oxime is a human 17α-hydroxylase/C17,20-lyase (P45017α) inhibitor with a human IC50 of 67 nM and a rat IC50 of 2754 nM. (3β)-3-(Acetyloxy)pregna-5,16-dien-20-one 20-oxime blocks the human testicular microsomal enzyme mediating androgen biosynthesis steps. (3β)-3-(Acetyloxy)pregna-5,16-dien-20-one 20-oxime does not inhibit human 5α-reductase in prostatic microsomes .
Synonyms: SKF-525A (Standard); U-5446 (Standard); RP-5171 (Standard)
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Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. 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 [4] .
Cat. No.: HY-159941
CAS No.: 2200453-71-8
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tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
Cat. No.: HY-181086
CAS No.: 2864394-30-7
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FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3 D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies .
Cat. No.: HY-16265A
CAS No.: 2514957-81-2
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JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
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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
