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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-162620
CAS No.: 2971825-58-6
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α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
Cat. No.: HY-169394
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5-HT1AR agonist 2 (Compound 4f) is a 5-HT1A receptor agonist (Ki: 10.0 nM). 5-HT1AR agonist 2 also binds to the SERT, D2 receptor and 5-HT6 receptor (Ki: SERT, 2.8 nM; D2, 23 nM; 5-HT6, 192 nM). 5-HT1AR agonist 2 is stabilized in microsomes and induces hypothermia in mice .
Cat. No.: HY-170491
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GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
Cat. No.: HY-172732
CAS No.: 3002409-47-1
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PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice .
Cat. No.: HY-182916
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NNRT-IN-16, Rilpivirin (HY-10574) analogue, is a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRT-IN-16 inhibits recombinant WT HIV-1 RT with an IC50 of 0.07 μM. NNRT-IN-16 exerts antiviral activity against wild-type and drug-resistant HIV-1 mutants, shows attenuated CYP isoenzyme and hERG inhibition, reduced cytotoxicity, and improved metabolic stability in human liver microsomes. NNRT-IN-16 can be used for the research of HIV-1 infection .
Cat. No.: HY-19153A
CAS No.: 157564-11-9
Synonyms: rel-TY-11345
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Nepaprazole sodium (rel-TY-11345) is a proton pump H+/K+-ATPase inhibitor. Nepaprazole sodium inhibits H+/K+-ATPase activity in rabbit gastric mucosal microsomes, with IC50 values of 5.8 μM and 9.9 μM at pH 6.0 and pH 7.4, respectively, and its inhibitory activity is enhanced under weakly acidic conditions. Nepaprazole sodium inhibits basal and Tetragastrin (HY-125556)-stimulated gastric acid secretion. Nepaprazole sodium can be used in studies on gastric proton pump function, gastric acid secretion, and mechanisms related to peptic ulcers .
Cat. No.: HY-101284A
CAS No.: 1031063-36-1
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(E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity .
Cat. No.: HY-170841
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HDAC3/BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3/BRD4 with an IC50 of 8 nM for HDAC3 (IC50s are 220 nM and 120 nM for HDAC1 and HDAC2, respectively). HDAC3/BRD4-IN-1 has anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3/BRD4-IN-1 in human liver microsomes is 29.36 min .
Cat. No.: HY-N3807S
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DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker DBCO-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. DBCO-PEG4-VC-PAB-DMEA-PNU-159682 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
Cat. No.: HY-155051
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Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
Cat. No.: HY-155141
CAS No.: 3003751-14-9
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hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
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-173024
CAS No.: 3053390-98-7
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TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
Cat. No.: HY-182800
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IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia .
Cat. No.: HY-B0822S1
Cat. No.: HY-134310
CAS No.: 1353586-18-1
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QC-308 hydrochloride 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 hydrochloride inhibits the activities of rat HO-1 and HO-2 in carbon monoxide generation assays using spleen and brain microsomes, respectively. QC-308 hydrochloride 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 hydrochloride is applicable for senescence-related research .
Cat. No.: HY-144123
CAS No.: 2719675-72-4
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
Cat. No.: HY-155050
Purity: 99.25%
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PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
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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
