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A1416712

Bindarit , ≥98% , 130641-38-2

CAS NO.:130641-38-2

Empirical Formula: C19H20N2O3

Molecular Weight: 324.37

MDL number: MFCD00866723

Pack Size Price Stock Quantity
5MG RMB396.80 In Stock
10MG RMB756.80 In Stock
50MG RMB2212.00 In Stock
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Update time: 2022-07-08

PRODUCT 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

Description and Uses

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.

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.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338

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