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经验配方 C₂₄H₁₉BFNO₅S 描述 概述 A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 µM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826 (Cat. No. 189510). 产品目录编号 189511 品牌系列 Calbiochem®
同义词 ATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid 参考 参考 Albers, H.M.H.G. et al. 2010. J. Med. Chem. 53, 4958.
Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA 107, 7257.产品信息 形式 Off-white solid Hill配方 C₂₄H₁₉BFNO₅S 化学配方 C₂₄H₁₉BFNO₅S Molar Mass 463.3 吸湿 Hygroscopic
结构配方图像 生物信息 纯度 ≥97% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
毒性 Regulatory Review
储存 -20°C
避光 Protect from light
吸湿 Hygroscopic
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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