Bindarit is an indazolic derivative with anti-inflammatory efficacy in vitro (150-300 μM) and in animal disease models in vivo (100 mg/kg ip, 50 mg/kg po, or 0.5% in chow; rats & mice). Bindarit selectively inhibits LPS-induced CCL2/MCP-1, CCL7/MCP-3, CCL8/MCP-2 chemokines over CCL3/MIP-1α and IL-8/CXCL8 in human monocytes, while blocking CCL2, but not CCL7 or CCL8, induction in HUVECs, and preventing LPS-induced CCL2 & IL-12β/p40 by inhibiting NFκB activation in murine macrophages (BMDM & Raw 264.7). Bindarit is also reported to exhibit non-competitive inhibiory potency against human monocarboxylate transporter MCT4 (Ki = 30.2 μM) over MCT1 (<40% inhibition at 500 μM).
Journal of neuroinflammation, 9, 171-171 (2012-07-14)
Production of the chemokine CCL2 by cells of the neurovascular unit (NVU) drives critical aspects of neuroinflammation. Suppression of CCL2 therefore holds promise in treating neuroinflammatory disease. Accordingly, we sought to determine if the compound bindarit, which inhibits CCL2 synthesis
Aims: Radiation-induced normal tissue toxicity often precludes the application of curative radiation doses. Here we investigated the therapeutic potential
β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate
Inflammation research : official journal of the European Histamine Research Society ... [et al.], 51(5), 252-258 (2002-06-12)
This study was designed to evaluate therapeutic effects of bindarit, an indazolic derivative able to inhibit monocyte chemoattractant protein-1 (MCP-1) production, in adjuvant induced arthritis in rats. Arthritis was induced by Freund's complete adjuvant injection. Bindarit was given as a
The activation of nuclear factor (NF)κB pathway and its transducing signaling cascade has been associated with the pathogenesis of many inflammatory diseases. The central role that IκBα and p65 phosphorylation play in regulating NFκB signalling in response to inflammatory stimuli
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