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

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.

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AMG-8718 Chemical Structure

AMG-8718 Chemical Structure

CAS No. : 1215868-94-2

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AMG-8718 Related Antibodies

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Description

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)

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].

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

AMG-8718 Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

442.44

Formula

C25H19FN4O3
CAS No.
SMILES

NC(OC1)=N[C@]1(C2=CC(C#CC3(C)COC3)=CN=C2O4)C5=C4C=CC(C6=CC=CN=C6F)=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AMG-8718 Related Classifications

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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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