AMG-8718

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510326

CAS#: 1215868-94-2

Description: AMG-8718 is a potent and orally efficacious BACE1 inhibitor. AMG-8718 produced robust and sustained reductions of CSF and brain Aβ levels in a rat pharmacodynamic model and exhibited significantly reduced potential for QTc elongation in a cardiovascular safety model. BACE1 (β-secretase, memapsin 2, Asp2) has emerged as a promising target for the treatment of Alzheimer's disease. BACE1 is an aspartic protease which functions in the first step of the pathway leading to the production and deposition of amyloid-β peptide (Aβ). BACE1 inhibition has direct implications in the Alzheimer's disease pathology without largely affecting viability.


Chemical Structure

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AMG-8718
CAS# 1215868-94-2

Theoretical Analysis

MedKoo Cat#: 510326
Name: AMG-8718
CAS#: 1215868-94-2
Chemical Formula: C25H19FN4O3
Exact Mass: 442.14412
Molecular Weight: 442.44
Elemental Analysis: C, 67.87; H, 4.33; F, 4.29; N, 12.66; O, 10.85

Size Price Shipping out time Quantity
Inquire bulk and customized quantity

Pricing updated 2021-02-28. Prices are subject to change without notice.

AMG-8718, is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Synonym: AMG8718; AMG 8718; AMG-8718.

IUPAC/Chemical Name: (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

InChi Key: GKKFBOARESVMBW-VWLOTQADSA-N

InChi Code: InChI=1S/C25H19FN4O3/c1-24(12-31-13-24)7-6-15-9-19-22(29-11-15)33-20-5-4-16(17-3-2-8-28-21(17)26)10-18(20)25(19)14-32-23(27)30-25/h2-5,8-11H,12-14H2,1H3,(H2,27,30)/t25-/m0/s1

SMILES Code: NC(OC1)=N[C@@]21C3=CC(C4=CC=CN=C4F)=CC=C3OC5=NC=C(C#CC6(C)COC6)C=C52

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 442.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Dineen TA, Chen K, Cheng AC, Derakhchan K, Epstein O, Esmay J, Hickman D, Kreiman CE, Marx IE, Wahl RC, Wen PH, Weiss MM, Whittington DA, Wood S, Fremeau RT Jr, White RD, Patel VF. 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. doi: 10.1021/jm5012676. Epub 2014 Nov 14. PubMed PMID: 25363711.

2: Fielden MR, Werner J, Jamison JA, Coppi A, Hickman D, Dunn RT 2nd, Trueblood E, Zhou L, Afshari CA, Lightfoot-Dunn R. Retinal Toxicity Induced by a Novel β-secretase Inhibitor in the Sprague-Dawley Rat. Toxicol Pathol. 2014 Oct 31. pii: 0192623314553804. [Epub ahead of print] PubMed PMID: 25361751.



Additional Information