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S80254

Verubecestat

源叶(MedMol) 99%
  • 英文名:
  • Verubecestat
  • 别名:
  • MK-8931; MK-8931-009; (R)-N-(3-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-4-fluorophenyl)-5-fluoropicolinamide; Verubecestat; MK8931; 2-Pyridinecarboxamide, N-[3-[(5R)-3-a
  • CAS号:
  • 1286770-55-5
  • 分子式:
  • C17H17F2N5O3S
  • 分子量:
  • 409.4104
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80254-5mg 99% ¥442.00元 10 - - - EA 加入购物车
源叶(MedMol) S80254-10mg 99% ¥666.40元 7 - - - EA 加入购物车
源叶(MedMol) S80254-25mg 99% ¥1292.00元 9 - - - EA 加入购物车
源叶(MedMol) S80254-100mg 99% ¥3264.00元 1 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease
  • 靶点: Ki: 2.2 nM (BACE1) and 0.38 nM (BACE2);Beta-Secretase;BACE
  • 体外研究:
    Verubecestat (MK-8931) is a β-site amyloid precursor protein cleaving enzyme 1/2 (BACE1/2) inhibitor. Verubecestat does not significantly inhibit human CYP isoforms 1A2, 2C9, 2C19, 2D6, and 3A4 (all IC50>40 μM), indicating that the compound is unlikely to be a perpetrator of CYP-mediated drug-drug interactions. Verubecestat has IC50s of 2.1 nM, 0.7 nM, 4.4 nM for Aβ1-40, Aβ1-42, sAPPβ in HEK293 APPSwe/Lon cells
  • 体内研究:
    Verubecestat (MK-8931; 3 mg/kg; IV or oral) has a T1/2 of 1.9 hours, a CL of 46 mL/min/kg, a Vss of 5.4 L/kg, a C max of 0.27 μM and a AUC of 1.1 μM•h for Sprague-Dawley (SD) rats.Verubecestat (1 mg/kg; IV) has a T1/2 of 4.9 hours, a CL of 21 mL/min/kg, a Vss of 7.5 L/kg for cynomolgus monkeys.Verubecestat (1 mg/kg; IV) has a T1/2 of 9.7 hours, a CL of 4.3 mL/min/kg, a Vss of 2.7 L/kg for beagle dogs.Verubecestat (30 mg/kg; orally; BID for 5 days) causes a modest (1.4-fold) induction of CYP 3A1 activity but does not significantly alter the expression of CYPs 1A1, 1A2, 2B, 3A2, or 4A in rats.Verubecestat dose-dependently reduces CSF and cortex Aβ40 with ED50 values of 5 and 8 mg/kg, respectively, corresponding to unbound plasma EC50 values of 48 and 81 nM, respectively.Verubecestat (3 and 10 mg/kg; orally) reduces profound, sustained of CSF Aβ40 levels and has peak effects on CSF Aβ lowering (72 and 81% reduction at 3 and 10 mg/kg, respectively) 12 h after dosing. Animal Model: Sprague-Dawley (SD) rats Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: IV or oral Result: Had a T1/2 of 1.9 hours, a CL of 46 mL/min/kg, a Vss of 5.4 L/kg, a Cmax of 0.27 μM and a AUC of 1.1 μM•h.
  • 参考文献:
    1. Scott JD, et al. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer'sDisease. Med Chem. 2016 Dec 8;59(23):10435-10450. 2. Yan R, et al. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.443 ml 12.213 ml 24.425 ml
    5 mM 0.489 ml 2.443 ml 4.885 ml
    10 mM 0.244 ml 1.221 ml 2.443 ml
    50 mM 0.049 ml 0.244 ml 0.489 ml
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