2. Neuronal Signaling
  3. Beta-secretase
  4. AMG-8718

AMG-8718 是一种有效的、选择性的和具有口服活性的 BACE1 抑制剂，对 BACE1 和 BACE2 的 IC50 值分别为 0.0007 和 0.005 µM。AMG-8718 显着降低 CSF 和大脑中的 Aβ40 水平。

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AMG-8718 Chemical Structure

AMG-8718 Chemical Structure

CAS No. : 1215868-94-2

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AMG-8718 相关抗体

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查看 Beta-secretase 亚型特异性产品:

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BACE1 BACE2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain[1].

IC50 & Target[1]

BACE1

0.0007 μM (IC50)

BACE2

0.005 μM (IC50)

体外研究
(In Vitro)

AMG-8718 (compound 42) shows good stability in human and rat liver microsomes, hERG binding activity with an Ki value of >10 µM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AMG-8718 相关抗体:
体内研究
(In Vivo)

AMG-8718 (compound 42) (10 mg/kg; p.o.)shows significantly decreases Aβ40 levels in the CSF and brain[1].
AMG-8718 (i.v. for 2 mg/kg or p.o. for 5 mg/kg) shows good bioavailability of 70%, 96%,101% for rats, beagle dog, monkey, respectively[1].
AMG-8718 (30 mg/kg for; p.o.) dose-dependent decreases in both CSF and brain Aβ levels at 4 h time points with 50% Aβ reduction (EC50) values of 18 and 67 nM for CSF and brain respectively in rats[1].
AMG-8718 (2.5, 8, 16 mg/kg; i.v.; a series of three 30 min infusions) shows high unbound plasma concentrations with 0.298, 1.70, 3.62 µM at the end of each infusion in chloralose-anesthetized dogs[1].
Pharmacokinetic Parameters ofAMG-8718 in rats, beagle dog, cynomolgus monkey[1].

species Cl (L/h/kg) Vdss(L/kg) t1/2(h) Cmax (µM) tmax(h) % F plasma protein binding (Fu)
i.v. p.o.
rat 0.33 1.1 4.8 3.8 1.7 70 0.013
beagle dog 0.26 1.6 5.2 8.1 1.0 96 0.038
monkey 0.61 2.2 7.7 6.1 1.7 101 0.054
2 mg/kg i.v.; rats (DMSO), dog (1% Tween80/2% HMPC/97% water at pH = 4), cynomolgus monkey (25% HBC/75% water at pH = 4); 5 mg/kg p.o. (1% Tween80/2% HMPC/97% water at pH = 2)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 10 mg/kg
Administration: Oral gavage
Result: Significantly decreased Aβ40 levels in the CSF at the 4 h time point at 69%, produced a robust response in the brain with 48% reduction of Aβ40 levels.
Animal Model: Rats, beagle dog, monkey[1]
Dosage: 2, 5 mg/kg
Administration: I.v. for 2 mg/kg or p.o. for 5 mg/kg
Result: Showed moderate total clearance, moderate Vdss, and half-lives of ca. 5-8 h across all three species, and bioavailability was high (70–101%).
Animal Model: Rats[1]
Dosage: 30 mg/kg
Administration: P.o.
Result: Demonstrated dose-dependent decreases in both CSF and brain Aβ levels at 4 h and 8 h time points.
分子量

442.44

Formula

C25H19FN4O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AMG-8718 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG-87181215868-94-2AMG8718AMG 8718Beta-secretaseBACEβ-Secretaseorally activeAβ40CSFbrainhERG bindingbioavailabilityInhibitorinhibitorinhibit

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