Bindarit
Bindarit Basic information
- Product Name:
- Bindarit
- Synonyms:
-
- Bindarit
- Propanoic acid, 2-Methyl-2-[[1-(phenylMethyl)-1H-indazol-3-yl]Methoxy]-
- 2-[(1-Benzyl-1H-indazol-3-yl)methoxy]-2-methylpropionic acid
- AF 2838
- 2-((1-Benzyl-1H-indazol-3-yl)Methoxy)-2-Methylpropanoic acid
- AF2838;AF-2838;AF 2838
- CS-1989
- 2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid
- CAS:
- 130641-38-2
- MF:
- C19H20N2O3
- MW:
- 324.37
- Product Categories:
-
- Aromatics
- Heterocycles
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 130641-38-2.mol
Bindarit Chemical Properties
- Boiling point:
- 542.9±40.0 °C(Predicted)
- Density
- 1.18±0.1 g/cm3 (20 ºC 760 Torr)
- storage temp.
- 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)
- color
- White to off-white
Bindarit Usage And Synthesis
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. 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-κB 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.
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.
Uses
Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
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