| Identification | Back Directory | [Name]
Bindarit | [CAS]
130641-38-2 | [Synonyms]
AF 2838
CS-1989
Bindarit
AF2838;AF-2838;AF 2838
2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid
2-[(1-Benzyl-1H-indazol-3-yl)methoxy]-2-methylpropionic acid
2-((1-Benzyl-1H-indazol-3-yl)Methoxy)-2-Methylpropanoic acid
Propanoic acid, 2-Methyl-2-[[1-(phenylMethyl)-1H-indazol-3-yl]Methoxy]- | [Molecular Formula]
C19H20N2O3 | [MDL Number]
MFCD00866723 | [MOL File]
130641-38-2.mol | [Molecular Weight]
324.37 |
| Chemical Properties | Back Directory | [Boiling point ]
542.9±40.0 °C(Predicted) | [density ]
1.18±0.1 g/cm3 (20 ºC 760 Torr) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:47.0(Max Conc. mg/mL);144.89(Max Conc. mM) | [form ]
A crystalline solid | [pka]
3.59±0.10(Predicted) |
| Hazard Information | Back Directory | [Description]
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.1 It inhibits LPS- or C. albicans-induced production of MCP-1/CCL2 in isolated human monocytes (IC50s = 172 and 403 μM, respectively).2 Bindarit downregulates NF-κB signaling and prevents p65 and p65/p50-mediated MCP-1/CCL2 promoter activation in RAW264.7 cells.3 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.4 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.5 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 MCT1.6 | [Uses]
Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. | [Uses]
Bindarit shows anti-inflammatory activity due to a selective inhibition of a subfamily of inflammatory chemokines. Bindarit is a also protein antidenaturant agent. Bindarit modulates the NFkB pathway and has been shown to reduce secondary phase of adjuvant arthritis in rats. |
|
|