ML353 是 mGlu5 沉默变构调节剂 (SAM) 的选择性配体,Ki 值为 18.2 nM。ML353 提高了常见变构位点的亲和力,比以前的 mGlu5 SAM 工具化合物 5mpep 高 20 倍。ML353 在解决 SAM 体内固有活性或作为一种药物阻断剂方面具有潜在应用。
生物活性
ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an K i value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a drug blocker.
性状
Solid
IC50 & Target[1][2]
mGlu5 18.2 nM (Ki)
体外研究(In Vitro)
ML353 是一种充分可溶性化合物,在 PBS 中的溶解度为 16.9 μM 或 6.0 μg/mL (PH=7.4)。ML353 在 PBS 缓冲液中具有优异的稳定性。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Gregory KJ, et al. Identification of a high affinity MPEP-site silent allosteric modulator (SAM) for the metabotropic glutamate subtype 5 receptor (mGlu5). 2013 Apr 15 [updated 2015 Feb 11]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–.