Bioactivity | BMS-932481 is an orally active modulator for γ-secretase, selectively reduce Aβ1-42 and Aβ1-40 production, with IC50s of 6.6 and 25.3 nM, respectively[1]. |
In Vivo | BMS-932481 (2-30 mg/kg,口服,单剂量) 在比格犬模型中可降低 Aβ1-42 和 Aβ1-40 的水平,增加 Aβ1-38 和 Aβ1-37 的水平,而不改变 Aβ 肽的总量[1]。BMS-932481 (2.5-15 mg/kg,静脉注射,单剂量) 具有中等的脑渗透性,在 Sprague-Dawley 大鼠模型中,脑与血浆比率和 AUCbrain 与 AUCplasma 比率约为 0.23 和 0.6[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 1263871-36-8 |
Formula | C24H24FN7O |
Molar Mass | 445.49 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Toyn JH, et al., Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects. J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. |