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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
38 Results for "
hepatocyte microsomes
" in MedChemExpress (MCE) Product Catalog:
Products (38)
38 Results for "hepatocyte microsomes" in MCE Product Catalog:
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2 Cited Publications
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KDM4C-IN-1 is a histone lysine demethylase KDM4C inhibitor with an IC50 of 8 nM. KDM4C-IN-1 inhibits cancer cell proliferation. KDM4C-IN-1 can be used in the research of hepatocellular carcinoma and adenocarcinoma alveolar basal epithelial carcinoma .
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1 Cited Publications
Cat. No.: HY-W795960
CAS No.: 108340-81-4
Synonyms: NT-814; BAY3427080
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Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
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ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11 .
Cat. No.: HY-160023
CAS No.: 2914919-85-8
Synonyms: D3S-001
Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
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PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
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Digoxigenin monodigitoxoside, a metabolite of Digoxin (HY-B1049), belongs to the class of cardenolides. Digoxigenin monodigitoxoside exerts its function by inhibiting Na,K-ATPase. Digoxigenin monodigitoxoside is used for the research of cardiovascular diseases such as congestive heart failure and cardiac arrhythmias .
Synonyms: PTC518
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Votoplam (PTC518) is a blood-brain barrier-permeable HTT pre-mRNA inhibitor with an IC50 ≤ 0.1 μM. Votoplam modulates the splicing process of HTT pre-mRNA to include a pseudo-exon carrying a premature translation termination codon, thereby triggering HTT mRNA degradation. Votoplam is applicable to research related to Huntington's disease .
Cat. No.: HY-19400
CAS No.: 284661-68-3
Synonyms: DPH-153893
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DPC-681 (DPH-153893) is an orally active HIV inhibitor. DPC-681 inhibits HIV protease activity and inhibits wild-type and mutant HIV replication. DPC-681 can be used for the research of HIV infection .
Synonyms: BAY 1902607
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Filapixant (BAY 1902607) is an orally active and selective P2X3 receptor antagonist. Filapixant is applicable to the research of refractory chronic cough .
Cat. No.: HY-121800
CAS No.: 1355243-24-1
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ML138 is a blood-brain barrier-permeable κ-opioid receptor (KOR) agonist, with an EC50 value of 0.87 μM and a human Ki value of 2.4 nM for human receptors; it exhibits high selectivity for KOR over μ, δ and other receptors. ML138 activates β-arrestin (beta-arrestin)-mediated signaling pathways, stimulates G protein coupling, and activates the downstream extracellular regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAP kinase) signaling pathway. ML138 is applicable to research related to addictive behaviors .
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TBA-354 is an orally active, blood-brain barrier permeable anti-tuberculosis compound . TBA-354 acts on replicating, non-replicating and drug-resistant Mycobacterium tuberculosis, retains its activity in the presence of serum proteins or albumin, and induces moderate, reversible neurotoxicity at effective dose levels. TBA-354 can be used in the research of tuberculosis and multidrug-resistant tuberculosis .
Cat. No.: HY-174443
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PROTAC sEH degrader-2 is a soluble epoxide hydrolase (sEH) PROTAC degrader, with pIC50 values of 8.37 and 7.12 against hsEH-H and msEH-H, respectively. PROTAC sEH degrader-2 induces targeted degradation of sEH via the ubiquitin-proteasome system, thereby completely blocking its dual functions as an epoxide hydrolase and a lipid phosphatase by bridging the short-branch exit of sEH with the CRBN E3 ubiquitin ligase. PROTAC sEH degrader-2 can be used in the research of neuroinflammation and Alzheimer's disease .
Cat. No.: HY-106379
CAS No.: 128486-54-4
Synonyms: GR-87442
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Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM. .
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MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
Cat. No.: HY-168956
Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 shows good metabolic stability in mouse liver microsomes and hepatocytes. Pks13-IN-2 can be used for tuberculosis research .
Cat. No.: HY-N11827
CAS No.: 22672-74-8
Synonyms: (+)-Isocorybulbine
Category:
Alkaloids Monophenols Phenols Plants Papaveraceae Alkaloid Dimers Corydalis turtschaninovii Bess.
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Cat. No.: HY-12485R
CAS No.: 1257426-19-9
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TBA-354 (Standard) is the analytical standard of TBA-354 (HY-12485). This product is intended for research and analytical applications. TBA-354 is an orally active, blood-brain barrier permeable anti-tuberculosis compound . TBA-354 acts on replicating, non-replicating and drug-resistant Mycobacterium tuberculosis, retains its activity in the presence of serum proteins or albumin, and induces moderate, reversible neurotoxicity at effective dose levels. TBA-354 can be used in the research of tuberculosis and multidrug-resistant tuberculosis .
Cat. No.: HY-162074
CAS No.: 2651908-78-8
Nipamovir is an orally active anti-HIV prodrug. Nipamovir is cleaved in vivo by glutathione and other active thiols. Nipamovir inhibits the replication of HIV-1RF and HIV-192HT599 in cells, with EC50 values of 3.64 μM and 3.23 μM, respectively. Nipamovir can be used in studies related to HIV infection .
Cat. No.: HY-184864
CAS No.: 2570323-59-8
HIV-IN-16 is a HIV replication inhibitor with an EC50 of 25 pM, and shows no activity in inducing CYP2B6. HIV-IN-16 inhibits HIV replication. HIV-IN-16 can be used in studies related to HIV infection and human immunodeficiency diseases .
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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
