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
此项目有
C Zoja et al.
Kidney international, 53(3), 726-734 (1998-03-21)
As an alternative to classical immunosuppressants in experimental lupus nephritis, we looked at bindarit, 2-methyl-2-[[1-phenylmethyl)-1H-indazol-3-y1]methoxy]propanoic acid, a novel molecule devoid of immunosuppressive effects, which selectively reduces chronic inflammation in rat adjuvant arthritis. Two groups of NZB/W mice (N = 55
Massimiliano Mirolo et al.
European cytokine network, 19(3), 119-122 (2008-09-09)
Bindarit is an indazolic derivative that is devoid of any immunosuppressive effects and has no effect on arachidonic acid metabolism. However, it has been proved to have anti-inflammatory activity in a number of experimental diseases, including pancreatitis, arthritis, and lupus
Xiaoming Cai et al.
Nature communications, 9(1), 4416-4416 (2018-10-26)
Increasing concerns over the possible risks of nanotechnology necessitates breakthroughs in structure-activity relationship (SAR) analyses of engineered nanomaterials (ENMs) at nano-bio interfaces. However, current nano-SARs are often based on univariate assessments and fail to provide tiered views on ENM-induced bio-effects. Here we
A Guglielmotti et al.
Clinical and experimental rheumatology, 16(2), 149-154 (1998-04-16)
The present study was designed to investigate the effects of bindarit on animal survival and renal damage in murine lupus autoimmune disease. Female NZB/W mice were used. Bindarit was administered, as a 0.5% medicated diet, starting either before the onset
Alina Wiesemann et al.
Antioxidants & redox signaling, 30(2), 213-231 (2018-02-22)
Aims: Radiation-induced normal tissue toxicity often precludes the application of curative radiation doses. Here we investigated the therapeutic potential
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