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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
61 Results for "
Microsomal stability
" in MedChemExpress (MCE) Product Catalog:
Products (61)
61 Results for "Microsomal stability" in MCE Product Catalog:
Cat. No.: HY-169429
CAS No.: 2568903-91-1
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CHIKV-IN-5 (Compound 26) is a CHIKV inhibitor (EC90 = 0.45 μM). CHIKV-IN-5 inhibits CHIKV replication at a late stage in the virus life cycle by blocking structural protein translation. CHIKV-IN-5 has great in vitro mouse microsomal stability. CHIKV-IN-5 reduces footpad swelling and decreases virus dissemination to other tissues in mice infected with CHIKV .
Cat. No.: HY-163403
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VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
Cat. No.: HY-155511
CAS No.: 3052383-83-9
DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance .
Cat. No.: HY-155512
CAS No.: 3052383-91-9
DprE1-IN-7 (Compound 64) is a DprE1 inhibitor. DprE1-IN-7 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-7 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-7 has high microsomal stability and medium clearance .
Cat. No.: HY-146057
CAS No.: 2411741-01-8
Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability .
Cat. No.: HY-159588
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Mcl-1 inhibitor 20 (compound 47) is a Mcl-1 inhibitor with anti-leukemic effects. Mcl-1 inhibitor 20 can bind to the BH3 binding groove of Mcl-1 (Ki=24 nM), occupy the P1 pocket in Mcl-1, and form interactions with Lys234 and Val249. Mcl-1 inhibitor 20 has good microsomal stability, pharmacokinetic characteristics and low cardiotoxicity .
Cat. No.: HY-178959
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FXR agonist 13 is a selective, orally active, potent FXR agonist (EC50 = 0.097 μM) and has favorable hepatic microsomal metabolic stability. FXR agonist 13 exhibits moderate affinity for FXR-LBD upon direct binding (KD = 14.74 μM). FXR agonist 13 displays good selectivity against related nuclear receptors, including LXRα/β, PPARα/γ/δ, PXR, and TGR5. FXR agonist 13 can be used for the study of metabolic-associated steatohepatitis (MASH) .
Cat. No.: HY-163799
CAS No.: 3048425-88-0
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PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
Cat. No.: HY-170887
CAS No.: 3094045-97-0
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MAO-B-IN-39 (compound11) is a selective monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-39 inhibits MAO-Bwith an IC50 of 3.61 μM. MAO-B-IN-39 demonstrates a potent NRF2 induction capacity. MAO-B-IN-39 exhibits potent anti-inflammatory and neuroprotective activity in OS (oxidative stress)-related in vitro models. MAO-B-IN-39 demonstrates high liver microsomal stability and favorable pharmacokinetics in mice. MAO-B-IN-39 is potential for Parkinson’s disease (PD) research .
Cat. No.: HY-163982
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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 .
Cat. No.: HY-178025
CAS No.: 3052313-53-5
TDI-014925 (Compound 58) is a SARS-CoV-2 methyltransferase nonstructural protein 14 (NSP14) inhibitor with an IC50 of 0.2 nM. TDI-014925 has an antiviral activity with significant microsomal stability and no CYP inhibitory activity. TDI-014925 can be used for COVID-19 research .
Cat. No.: HY-179639
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PDE4-IN-30 is a selective PDE4 inhibitor with an IC50 of 2.7 nM for PED4D2, targeting PDE4 through halogen bonding and metal coordination. PDE4-IN-30 exhibits at least 67-fold selectivity for other PDE subfamilies. PDE4-IN-30 can be used for the research of idiopathic pulmonary fibrosis .
Cat. No.: HY-180403
CAS No.: 3032232-47-3
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TLX agonist 3 is a potent and selective tailless homolog (TLX, NR2E1) agonist with an EC50 of 0.25 μM and a Kd of 1.6 μM). TLX agonist 3 shows high selectivity over related nuclear receptors, and promotes TLX oligomerization with an EC50 of 5.0 μM. TLX agonist 3 can be used for the research of neurodegenerative diseases .
Cat. No.: HY-182042
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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-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 .
Cat. No.: HY-123882
CAS No.: 1604034-78-7
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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-182244
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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-182355
CAS No.: 3125953-23-0
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MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
Cat. No.: HY-123599
CAS No.: 1884209-98-6
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IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target .
Cat. No.: HY-182356
CAS No.: 3125953-25-2
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MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .
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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
