A high-affinity ligand of A-FABP/aP2 (Ki = 0.67 μM); shown to antagonize the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes; presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2

HTS 01037 – 5 mg

Brand:
Cayman
CAS:
682741-29-3
Storage:
-20
UN-No:
Non-Hazardous - /

Adipocyte fatty acid binding protein (A-FABP/aP2) is a carrier protein expressed in both adipocytes and macrophages where it functions in intracellular fatty acid solubilization, trafficking, and metabolism.{11977} Molecular disruption of A-FABP/aP2 in mice results in improved insulin sensitivity and protection from atherosclerosis.{12288,14840} HTS 01037 is a high-affinity ligand of adipocyte fatty acid binding protein (A-FABP/aP2) (Ki = 0.67 μM) that presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2.{18878} At a concentration of 10 μM, HTS 01037 antagonizes the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes. {18878} HTS 01037 inhibits lipolysis in 3T3L1 adipocytes and reduces lipopolysaccharide-stimulated inflammation in bone marrow-derived macrophages, both effects of which are similar to the phenotype of A-FABP/aP2 knockout mice.{18878}  

 

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SKU: 10699 - 5 mg Category:

Description

A high-affinity ligand of A-FABP/aP2 (Ki = 0.67 μM); shown to antagonize the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes; presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2

Formal name: 4-[(3-carboxy-1-oxo-2-propen-1-yl)amino]-[2,2′-bithiophene]-5-carboxylic acid, 5-methyl ester

Synonyms: 

Molecular weight: 337.4

CAS: 682741-29-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area

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