GS967
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MedKoo CAT#: 510345

CAS#: 1262618-39-2

Description: GS967, also known as GS-458967, is a highly selective late sodium channel current blocker. The selective inhibition of late INa with GS967 can exert antiarrhythmic effects by suppressing EAD- and DAD-mediated extrasystolic activity in PFs and PV and SVC sleeve preparations. Selective late INa inhibition with GS967 exerts potent protective effects against ischemia-induced depolarization and repolarization abnormalities in both atria and ventricles.


Chemical Structure

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GS967
CAS# 1262618-39-2

Theoretical Analysis

MedKoo Cat#: 510345
Name: GS967
CAS#: 1262618-39-2
Chemical Formula: C14H7F6N3O
Exact Mass: 347.04933
Molecular Weight: 347.22
Elemental Analysis: C, 48.43; H, 2.03; F, 32.83; N, 12.10; O, 4.61

Size Price Shipping out time Quantity
5mg USD 85 Same day
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 650 Same day
200mg USD 1050 Same day
500mg USD 1950 2 weeks
1g USD 2950 2 weeks
2g USD 5250 2 weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-07. Prices are subject to change without notice.

GS967, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: GS967; GS-967; GS 967; GS458967; GS 458967; GS-458967

IUPAC/Chemical Name: 6-(4-(trifluoromethoxy)phenyl)-3-(trifluoromethyl)(1,2,4)triazolo(4,3-a)pyridine

InChi Key: FEVBKJITJDHASC-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H7F6N3O/c15-13(16,17)12-22-21-11-6-3-9(7-23(11)12)8-1-4-10(5-2-8)24-14(18,19)20/h1-7H

SMILES Code: FC(C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21)(F)F

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO, not in water 100.0

Preparing Stock Solutions

The following data is based on the product molecular weight 347.22 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: Bonatti R, Silva AF, Batatinha JA, Sobrado LF, Machado AD, Varone BB, Nearing BD, Belardinelli L, Verrier RL. Selective late sodium current blockade with GS-458967 markedly reduces ischemia-induced atrial and ventricular repolarization alternans and ECG heterogeneity. Heart Rhythm. 2014 Oct;11(10):1827-35. doi: 10.1016/j.hrthm.2014.06.017. Epub 2014 Jun 17. PubMed PMID: 24953379.

2: Anderson LL, Thompson CH, Hawkins NA, Nath RD, Petersohn AA, Rajamani S, Bush WS, Frankel WN, Vanoye CG, Kearney JA, George AL Jr. Antiepileptic activity of preferential inhibitors of persistent sodium current. Epilepsia. 2014 Aug;55(8):1274-83. doi: 10.1111/epi.12657. Epub 2014 May 23. PubMed PMID: 24862204; PubMed Central PMCID: PMC4126848.

3: Fernandes S, Hoyer K, Liu G, Wang WQ, Dhalla AK, Belardinelli L, Rajamani S. Selective inhibition of the late sodium current has no adverse effect on electrophysiological or contractile function of the normal heart. J Cardiovasc Pharmacol. 2014 Jun;63(6):512-9. doi: 10.1097/FJC.0000000000000075. PubMed PMID: 24406487.

4: Pezhouman A, Madahian S, Stepanyan H, Ghukasyan H, Qu Z, Belardinelli L, Karagueuzian HS. Selective inhibition of late sodium current suppresses ventricular tachycardia and fibrillation in intact rat hearts. Heart Rhythm. 2014 Mar;11(3):492-501. doi: 10.1016/j.hrthm.2013.11.026. Epub 2013 Nov 28. PubMed PMID: 24291413; PubMed Central PMCID: PMC3963462.

5: Trenor B, Gomis-Tena J, Cardona K, Romero L, Rajamani S, Belardinelli L, Giles WR, Saiz J. In silico assessment of drug safety in human heart applied to late sodium current blockers. Channels (Austin). 2013 Jul-Aug;7(4):249-62. PubMed PMID: 23696033; PubMed Central PMCID: PMC3989354.

6: Sicouri S, Belardinelli L, Antzelevitch C. Antiarrhythmic effects of the highly selective late sodium channel current blocker GS-458967. Heart Rhythm. 2013 Jul;10(7):1036-43. doi: 10.1016/j.hrthm.2013.03.023. Epub 2013 Mar 22. PubMed PMID: 23524321; PubMed Central PMCID: PMC3836836.

7: Belardinelli L, Liu G, Smith-Maxwell C, Wang WQ, El-Bizri N, Hirakawa R, Karpinski S, Li CH, Hu L, Li XJ, Crumb W, Wu L, Koltun D, Zablocki J, Yao L, Dhalla AK, Rajamani S, Shryock JC. A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32. doi: 10.1124/jpet.112.198887. Epub 2012 Sep 25. PubMed PMID: 23010360.

 



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