Bindarit

Bindarit is an inhibitor of monocyte chemoattractant protein (MCP) production that is selective for MCP-1/CCL2, MPC-3/CCL7, and MCP-2/CCL8 over other chemokines. It inhibits LPS- or C. albicans-induced production of MCP-1/CCL2 in isolated human monocytes (IC50s = 172 and 403 µM, respectively). Bindarit downregulates NF-kappaB signaling and prevents p65 and p65/p50-mediated MCP-1/CCL2 promoter activation in RAW264.7 cells. It delays the onset of proteinuria and prolongs survival in a mouse model of experimental lupus nephritis when administered at a dose of 50 mg/kg. It prevents LPS-induced increases in MCP-1/CCL2 expression in mouse brain and spinal cord when administered at a dose of 200 mg/kg and reduces the incidence and severity of experimental autoimmune encephalomyelitis (EAE) in mice. Bindarit is also a noncompetitive inhibitor of monocarboxylate transporter 4 (MCT4, Ki = 30.2 µM for the human transporter) that is selective for MCT4 over MCT1.Formal Name: 2-methyl-2-[[1-(phenylmethyl)-1H-indazol-3-yl]methoxy]-propanoic acid. CAS Number: 130641-38-2. Synonyms: AF 2838. Molecular Formula: C19H20N2O3. Formula Weight: 324.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 20 mg/ml. lambdamax: 209, 294 nm. SMILES: OC(C(C)(C)OCC1=NN(CC2=CC=CC=C2)C3=CC=CC=C31)=O. InChi Code: InChI=1S/C19H20N2O3/c1-19(2,18(22)23)24-13-16-15-10-6-7-11-17(15)21(20-16)12-14-8-4-3-5-9-14/h3-11H,12-13H2,1-2H3,(H,22,23). InChi Key: MTHORRSSURHQPZ-UHFFFAOYSA-N.