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| 品牌 | absin | CAS | 1262036-50-9 |
|---|---|---|---|
| 分子式 | C18H16F2N4O2S | 纯度 | ＞98% |
| 分子量 | 390.41 | 货号 | abs810333 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | used for the treatment of Alzheimer's Di | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
LY2886721 1262036-50-9
| 产品描述 | |
| 描述 | LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | LY 2886721,LY-2886721,N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 9 mg/mL (23.05 mM) |
| 生物活性 | |
| 靶点 | BACE2 ,BACE1 |
| In vitro(体外研究) | LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the clinical progression of AD. LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid. LY2886721 inhibits recombinant hBACE1 with an IC50 of 20.3 nM. In cellular assays, LY2886721 inhibits Abeta with an IC50 of 18.7 nM and 10.7 nM, HEK293Swe and PDAPP neuronal culture, respectively. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid β lowering in nonclinical animal models. Assessment of LY2886721 activity against hBACE2 demonstrates an IC50 of 10.2 nM. Assessment of LY2886721 activity against cathepsin D, pepsin, renin, or other important aspartyl proteases shows essentially no inhibition (IC50 >100,000 nM), suggesting that activity against these common aspartyl proteases is unlikely to be significant. |
| In vivo(体内研究) | Oral administration of LY2886721 to PDAPP mice produces dose-dependent reductions in brain Abeta, C99 and sAPPbeta. Brain Abeta levels are decreased ∼20%-65% relative to vehicle-treated groups three hours after a 3-30 mg/kg dose of LY2886721. Brain C99 and sAPPb levels also are reduced in a dose-dependent manner consistent with BACE1 inhibition in vivo. The pharmacodynamic responses to LY2886721 persists out to 9 hours post dose in brains of PDAPP mice. Pharmacodynamic studies in beagle dog reveal robust and sustained reductions in plasma Abeta following 1 mg/kg LY2886721 dosing. Central effects of BACE1 inhibition in dog are manifested by a 50% reduction in CSF Abeta at 9 hours after a 0.5 mg/kg dose of LY2886721. The geometric mean terminal elimination t1/2 is determined to be 17.2 h (range 8.19-36.3 h). The geometric mean apparent oral clearance is 34.8 L/h (38% CV) and the apparent volume of distribution during the terminal phase was 863 L (56% CV) across dose levels. LY2886721 is freely permeable across the blood-brain barrier. |
| 研究领域 | |
| 研究领域 | Proteolysis / UbiquitinProteolytic enzymesAspartic proteaseBACEs NeuroscienceDiseases NeuroscienceNeurology processNeurodegenerative diseaseAlzheimer's diseaseProteases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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