SML2910
Bindarit
≥98% (HPLC)
别名:
2-((1-Benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid, 2-Methyl-2-[[1-(phenylmethyl)-1H-indazol-3-yl]methoxy]propanoic acid, AF 2838, AF2838
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
[n]2(nc(c3c2cccc3)COC(C)(C)C(=O)O)Cc1ccccc1
InChI
1S/C19H20N2O3/c1-19(2,18(22)23)24-13-16-15-10-6-7-11-17(15)21(20-16)12-14-8-4-3-5-9-14/h3-11H,12-13H2,1-2H3,(H,22,23)
InChI key
MTHORRSSURHQPZ-UHFFFAOYSA-N
相关类别
生化/生理作用
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).
NFκB activation, CCL2 (MCP1) & IL-12β/p40 induction blocker with anti-inflammation efficacy in vivo. Selectively inhibits monocarboxylate transporter MCT4 over MCT1.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Guo-Xiong Zhou et al.
Hepatobiliary & pancreatic diseases international : HBPD INT, 9(2), 201-207 (2010-04-13)
Chemokines and their receptors play key roles in the pathogenesis of acute pancreatitis. This study aimed to establish a rat model of severe acute pancreatitis (SAP) for investigating monocyte chemotactic protein-1 (MCP-1) expression in the pathogenesis of the disease. We
Yuya Futagi et al.
Biochemical and biophysical research communications, 495(1), 427-432 (2017-10-11)
The human monocarboxylate transporters (hMCTs/SLC16As) mediate the uptake of various monocarboxylates. Several isoforms of hMCTs are expressed in cancerous tissue as well as in normal tissue. In cancerous tissue, hypoxia induces the expression of hMCT4, which transports the energetic metabolite
Shujun Ge et al.
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
Jiro Ogura et al.
Pharmaceutical research, 36(6), 84-84 (2019-04-19)
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
A Guglielmotti et al.
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
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