AMG-8718

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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.

For research use only. We do not sell to patients.

AMG-8718 Chemical Structure

CAS No. : 1215868-94-2

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BACE1 BACE2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

BACE1

0.0007 μM (IC₅₀)

BACE2

0.005 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	4.4 nM Compound: 42, AMG-8718	Inhibition of BACE1 in HEK293 cells assessed as Abeta40 level after overnight incubation by sandwich ELISA Inhibition of BACE1 in HEK293 cells assessed as Abeta40 level after overnight incubation by sandwich ELISA	[PMID: 25363711]

In Vitro

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

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

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)	V_dss(L/kg)	t_1/2(h)	C_max (µM)	t_max(h)	% F	plasma protein binding (F_u)
	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.

1215868-94-2

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

Handling Instructions (2659 KB)

References

[1]. Dineen TA,et al. Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718). J Med Chem. 2014 Dec 11;57(23):9811-31. [Content Brief]

AMG-8718 Related Classifications

Neurological Disease

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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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