Scientific Reviews
Product Guides
Blogs
Topics
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
41 Results for "
low clearance
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "low clearance" in MCE Product Catalog:
15
15 Publications Verification
Research Areas:
p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
7
7 Cited Publications
Cat. No.: HY-D1063
CAS No.: 207399-07-3
5
5 Cited Publications
Target:
Research Areas:
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 .
1
1 Cited Publications
JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties .
Cat. No.: HY-112624B
CAS No.: 9004-54-0
Synonyms: Dextran 70; Dextran D70; Dextran T70(MW 64000-76000)
Research Areas:
Colesevelam hydrochloride is an orally active bile acid sequestrant, lipid-lowering agent, and glycemic control agent. Colesevelam hydrochloride binds bile acids in the gastrointestinal tract to form nonabsorbable complexes, interrupts enterohepatic recirculation and increases fecal bile acid elimination. Colesevelam hydrochloride modulates FXR, TGR5, and Cyp7a1 activity and triggers cAMP signaling and GLP-1 release. Colesevelam hydrochloride alters hepatic lipid and glucose metabolism, suppresses hepatic glycogenolysis, reduces hepatic triglyceride and cholesterol levels, and increases LDL-C (low-density lipoprotein cholesterol) clearance. Colesevelam hydrochloride can be used for the research of type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease .
Cat. No.: HY-112624E
CAS No.: 9004-54-0
Synonyms: Dextran 0.8; Dextran D0.8; Dextran T0.8(MW 640-960)
Target:
Research Areas:
Gcase activator 2 (compound 14), a pyrrolo[2,3-b]pyrazine, is alos a β-Glucocerebrosidase (GCase) activator (EC50=3.8 μM). Gcase activator 2 induces GCase dimerizatio (both K-type and V-type). And Gcase activator 2 has low metabolic clearance in human and mouse .
Cat. No.: HY-117912
CAS No.: 1431553-15-9
Target:
Research Areas:
TRC210258 is a TGR5 agonist with activity to improve diabetes-associated hyperglycemia and dyslipidemia. TRC210258 promotes energy expenditure by enhancing the release of glucagon-like peptide-1. TRC210258 is able to improve glucose metabolic control in high-fat diet-induced obese mice. TRC210258 also showed improvement in lipid parameters in high-fat-fed hamsters, including reductions in plasma triglyceride and low-density lipoprotein cholesterol levels. TRC210258 improved emerging lipid-related cardiovascular risk parameters including remnant cholesterol and triglyceride clearance .
Cat. No.: HY-173006
CAS No.: 2893978-54-4
Target:
Research Areas:
AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 of < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound that can be used for the study of breast cancer .
Cat. No.: HY-163476
CAS No.: 3060954-15-3
Target:
Research Areas:
PIP5K1C-IN-1 (Compound 30) is a potent PIP5K1C inhibitor, with an IC50 of 0.80 nM. PIP5K1C-IN-1 exhibits low total clearance in mice and high levels of kinase selectivity. PIP5K1C-IN-1 can be used for the research of cancer and chronic pain .
Cat. No.: HY-143255
CAS No.: 2631703-04-1
Target:
Research Areas:
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
Cat. No.: HY-162459
CAS No.: 3036368-70-1
Target:
Research Areas:
cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats .
Cat. No.: HY-162238
CAS No.: 2650846-59-4
OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
Target:
Research Areas:
GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
Cat. No.: HY-12733
CAS No.: 1254318-44-9
Target:
Research Areas:
AZD5248 is an orally active, selective dipeptidyl peptidase 1 (cathepsin C) inhibitor, with IC50 values of 1 nM and 17 nM against human CatC, 44 nM against human DPP1, and 67 nM against rat DPP1. It exhibits low clearance and high bioavailability in animal models. AZD5248 forms an irreversible covalent bond with the catalytic Cys234 residue of CatC, exerts reversible inhibition via its nitrile moiety, blocks CatC-dependent amyloid formation, and reduces the activation levels of neutrophil serine proteases in bone marrow and blood. AZD5248 reacts with aortic elastin aldehydes to form stable 4-imidazolinones, induces ultrastructural changes in aortic tissue, and has an α-amino acid-based backbone. AZD5248 reduces the severity of acute pancreatitis in mouse models. AZD5248 can be used in research on chronic obstructive pulmonary disease, acute pancreatitis, neurodegenerative diseases, lysosomal storage disorders, acute lung injury, cystic fibrosis, and neutrophil-mediated inflammatory diseases .
Cat. No.: HY-120004
CAS No.: 2115022-67-6
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
Cat. No.: HY-119216
CAS No.: 2016806-55-4
AZ13711265 is an orally active PAK1 inhibitor with high selectivity. AZ13711265 has IC50 values of 0.58 nM and 0.11 µM for PAK1 and pPAK1, respectively. AZ13711265 has low lipophilicity and low clearance, and can be used as an in vivo probe compound for PAK1. AZ13711265 can be used in the study of cancer .
Cat. No.: HY-112047
CAS No.: 1423007-82-2
Synonyms: GSK2878175
GSK8175 is a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV). GSK8175 is a sulfonamide- N-benzoxaborole analog with low in vivo clearance across preclinical species and broad-spectrum activity against HCV replicons .
Cat. No.: HY-116494
CAS No.: 1699720-89-2
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
-
-
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
