S84286 |
BMT-145027 |
源葉(MedMol) | 98% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM
- 靶點: mGluR5:47 nM (EC50);GluR
- 體外研究:
BMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC50=47 nM), and a modest decrease in planarity (Fsp3 = 0.17). Importantly, BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM
- 體內(nèi)研究:
Drug-treated and control mice are shown two identical objects. After a 24-h natural forgetting period, the mice are reintroduced to a familiar object while simultaneously presented with a novel object. Since mice spend more time exploring unfamiliar objects, improved memory is measured as time spent exploring the novel object. BMT-145027 leads to a significant increase in time spent with the novel object when dosed at 30 mg/kg, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals indicates a total plasma concentration of 2800 nM at 30 mg/kg
- 參考文獻:
1. Hill MD, et al. Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086.
- 溶解性: Soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.279 ml 11.394 ml 22.788 ml 5 mM 0.456 ml 2.279 ml 4.558 ml 10 mM 0.228 ml 1.139 ml 2.279 ml 50 mM 0.046 ml 0.228 ml 0.456 ml
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)