| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S80254-5mg | 99% | ￥442.00元 | 10 | - | - | - |
|
| 源叶(MedMol) | S80254-10mg | 99% | ￥666.40元 | 7 | - | - | - |
|
| 源叶(MedMol) | S80254-25mg | 99% | ￥1292.00元 | 8 | - | - | - |
|
| 源叶(MedMol) | S80254-100mg | 99% | ￥3264.00元 | 1 | - | - | - |
|
| 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：
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
|---|
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京