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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
12 Results for "
intrinsic clearance
" in MedChemExpress (MCE) Product Catalog:
Products (12)
12 Results for "intrinsic clearance" in MCE Product Catalog:
5
5 Cited Publications
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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
Synonyms: Genistein 7-O-glucuronide
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Genistein 7-β-D-Glucuronide (Genistein 7-O-glucuronide) is the primary phase II metabolite of Genistein (HY-14596) in human and rat hepatocytes. Genistein 7-β-D-Glucuronide undergoes distinct deconjugation in different functional assays. Genistein 7-β-D-Glucuronide is produced via hepatic microsomal glucuronidation and shows a mild age-related increase in intrinsic clearance in male F344 rats. Genistein 7-β-D-Glucuronide can be used for research on metabolism .
Cat. No.: HY-175207
CAS No.: 3109469-27-1
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CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .
Cat. No.: HY-148075
CAS No.: 2365241-79-6
PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ, with a mean pIC50 value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum .
Cat. No.: HY-170973
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KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
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ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research .
Cat. No.: HY-178282
CAS No.: 2169271-17-2
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JAK1-IN-19 (Compound 18) is a potent JAK1 inhibitor with IC50s of 0.02, 0.5, 91 and 0.2 nM against JAK1, JAK2, JAK3 and TYK2. JAK1-IN-19 exhibits improved rat and human intrinsic clearance. JAK1-IN-19 can be used for the studies of atopic dermatitis and other autoimmune diseases .
Cat. No.: HY-146113
CAS No.: 2667681-85-6
IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .
Cat. No.: HY-146111
CAS No.: 2667681-57-2
IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg .
Cat. No.: HY-W413619
CAS No.: 1193314-24-7
Synonyms: NITD609 enantiomer; KAE609 enantiomer
Cipargamin enantiomer (NITD609 enantiomer) is a Plasmodium falciparum inhibitor that can be characterized as a spirotetrahydro β-carboline (1S,3R stereoisomer). Cipargamin enantiomer exerts antiplasmodial activity against Plasmodium falciparum strains NF54 (IC50 of 77 nM) and K1. Cipargamin enantiomer displays low liver microsomal intrinsic clearance in mouse and human systems. Cipargamin enantiomer does not inhibit CYP2C9. Cipargamin enantiomer can be used for the research of malaria .
Cat. No.: HY-100432R
CAS No.: 877963-94-5
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LOC14 (Standard) is the analytical standard of LOC14 (HY-100432). This product is intended for research and analytical applications. LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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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
