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MedKoo Cat#: 526976 | Name: GS-462808

Description:

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

GS-462808 is a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms. GS-462808 has an improved CNS window , and improved anti-ischemic potency relative to ranolazine.

Chemical Structure

GS-462808
GS-462808
CAS#1354198-41-6

Theoretical Analysis

MedKoo Cat#: 526976

Name: GS-462808

CAS#: 1354198-41-6

Chemical Formula: C17H12F3N5O3

Exact Mass: 391.0892

Molecular Weight: 391.31

Elemental Analysis: C, 52.18; H, 3.09; F, 14.57; N, 17.90; O, 12.27

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
GS-462808; GS 462808; GS462808.
IUPAC/Chemical Name
2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one
InChi Key
CIUYUJJQZDDGTM-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H12F3N5O3/c1-10-21-15(28-23-10)9-25-16(26)24-8-12(4-7-14(24)22-25)11-2-5-13(6-3-11)27-17(18,19)20/h2-8H,9H2,1H3
SMILES Code
O=C1N(CC2=NC(C)=NO2)N=C3C=CC(C4=CC=C(OC(F)(F)F)C=C4)=CN31
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
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 391.31 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.

Recalculate based on batch purity %
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
1: Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Hirakawa R, Smith-Maxwell C, Wu L, Dhalla AK, Rajamani S, Mollova N, Stafford B, Tang J, Belardinelli L, Zablocki JA. Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3207-11. doi: 10.1016/j.bmcl.2016.03.096. Epub 2016 Mar 26. PubMed PMID: 27038498.