An inhibitor of MCP production; selective for MCP-1/CCL2

Bindarit – 5 mg

Brand:
Cayman
CAS:
130641-38-2
Storage:
-20
UN-No:
Non-Hazardous - /

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.{49037} It inhibits LPS- or C. albicans-induced production of MCP-1/CCL2 in isolated human monocytes (IC50s = 172 and 403 µM, respectively).{30874} Bindarit downregulates NF-κB signaling and prevents p65 and p65/p50-mediated MCP-1/CCL2 promoter activation in RAW264.7 cells.{30873} 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.{30875} 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.{30872} 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.{43672}  

 

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SKU: 11479 - 5 mg Category:

Description

An inhibitor of MCP production; selective for MCP-1/CCL2, MPC-3/CCL7, and MCP-2/CCL8; inhibits LPS- or C. albicans-induced production of MCP-1/CCL2 in isolated human monocytes (IC50s = 172 and 403 µM, respectively); delays the onset of proteinuria and prolongs survival in a mouse model of experimental lupus nephritis at 50 mg/kg; prevents LPS-induced increases in MCP-1/CCL2 expression in mouse brain and spinal cord when administered at a dose of 200 mg/kg; a noncompetitive inhibitor of MCT4 (Ki = 30.2 µM) that is selective for MCT4 over MCT1

Formal name: 2-methyl-2-[[1-(phenylmethyl)-1H-indazol-3-yl]methoxy]-propanoic acid

Synonyms:  AF 2838

Molecular weight: 324.4

CAS: 130641-38-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Immunology & Inflammation|Autoimmunity|Lupus||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience

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