LY2886721 is a potent, selective and orally activebeta-site amyloid precursor protein cleaving enzyme 1 (BACE1)inhibitor with anIC₅₀of 20.3 nM for recombinant humanBACE1. LY2886721 is selectivity againstcathepsin D, pepsin, andrenin, but lacking selectivity againstBACE2(IC₅₀of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment^[1].

IC50: 20.3 nM (Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)); 10.2 nM (BACE2)^[1]

Overnight exposure of HEK293Swe cells to increasing concentrations of LY2886721 shows a concentration-dependent decrease in the amount of Aβ secreted into the condition medium. Consistent with a mechanism of BACE inhibition, the EC₅₀s for inhibition of Aβ_1-40and Aβ_1-42are essentially identical, 18.5 and 19.7 nM, respectively^[1].
Overnight exposure of PDAPP neuronal cultures to an increasing concentration of LY2886721 produces a concentration-dependent decrease in Aβ production. As observed in HEK293Swe cells, the EC₅₀s for inhibition of Aβ_1-40and Aβ_1-42are comparable in PDAPP neuronal cultures at ~10 nM^[1].

LY2886721 (3-30 mg/kg; oral administration; PDAPP mice) treatment significantly reduces the hippocampal and cortical levels of Aβ_1-x. LY2886721 treatment results in significant reduction of brain parenchymal levels of C99 and sAPPβ^[1].

390.41

Solid

C₁₈H₁₆F₂N₄O₂S

1262036-50-9

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 16.67 mg/mL(42.70 mM)

H₂O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2 mg/mL (5.12 mM); Clear solution

  此方案可获得 ≥ 2 mg/mL (5.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。