WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H556140
CAS#: 866760-23-8 (HBr)
Description: F 15845 is a blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. F15845 has been shown to selectively inhibit the persistent sodium current of Nav1.5[1] exerting cardioprotective effects following ischemia. In vitro testing showed minimal effects of F15845 on other important ion channels of the heart, including major Ca2+ and K+ channels.[1] This characteristic is thought to account for the limited effect of F15845 to change other heart parameters such as basal cardiac function, hemodynamic functions and ventricular fibrillation. F15845 was also shown to exert improved effects when the membrane potential was depolarized,[1] by acting on the extracellular side of the channel.
Hodoodo Cat#: H556140
Name: F15845 HBr
CAS#: 866760-23-8 (HBr)
Chemical Formula: C20H26BrNO2S2
Exact Mass: 0.00
Molecular Weight: 456.457
Elemental Analysis: C, 52.63; H, 5.74; Br, 17.51; N, 3.07; O, 7.01; S, 14.05
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Related CAS #: 470454-73-0 (free base) 866760-23-8 (HBr) 470454-74-1 (fumarate)
Synonym: F15845 HBr; F15845 hydrobromide; F15845; F-15845; F 15845;
IUPAC/Chemical Name: (S)-N-((S)-3-((2-methoxyphenyl)thio)-2-methylpropyl)-3,4-dihydro-2H-benzo[b][1,4]oxathiepin-3-amine hydrobromide
InChi Key: CUWFVJMNULNBTG-MOGJOVFKSA-N
InChi Code: InChI=1S/C20H25NO2S2.BrH/c1-15(13-24-19-9-5-3-7-17(19)22-2)11-21-16-12-23-18-8-4-6-10-20(18)25-14-16;/h3-10,15-16,21H,11-14H2,1-2H3;1H/t15-,16-;/m0./s1
SMILES Code: C[C@H](CSC1=CC=CC=C1OC)CN[C@H]2COC3=CC=CC=C3SC2.[H]Br
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 456.46 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.
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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Antzelevitch C, Nesterenko V, Shryock JC, Rajamani S, Song Y, Belardinelli L. The role of late I Na in development of cardiac arrhythmias. Handb Exp Pharmacol. 2014;221:137-68. doi: 10.1007/978-3-642-41588-3_7. PMID: 24737235; PMCID: PMC4076160.
2: Bocquet A, Sablayrolles S, Vacher B, Le Grand B. F 15845, a new blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. Br J Pharmacol. 2010 Sep;161(2):405-15. doi: 10.1111/j.1476-5381.2010.00912.x. PMID: 20735424; PMCID: PMC2989591.
3: Pignier C, Rougier JS, Vié B, Culié C, Verscheure Y, Vacher B, Abriel H, Le Grand B. Selective inhibition of persistent sodium current by F 15845 prevents ischaemia-induced arrhythmias. Br J Pharmacol. 2010 Sep;161(1):79-91. doi: 10.1111/j.1476-5381.2010.00884.x. PMID: 20718741; PMCID: PMC2962818.
4: Létienne R, Bel L, Bessac AM, Vacher B, Le Grand B. Myocardial protection by F 15845, a persistent sodium current blocker, in an ischemia-reperfusion model in the pig. Eur J Pharmacol. 2009 Dec 10;624(1-3):16-22. doi: 10.1016/j.ejphar.2009.09.032. Epub 2009 Sep 22. PMID: 19778535.
5: Vié B, Sablayrolles S, Létienne R, Vacher B, Darmellah A, Bernard M, Feuvray D, Le Grand B. 3-(R)-[3-(2-methoxyphenylthio-2-(S)-methylpropyl]amino-3,4-dihydr o-2H-1,5-benzoxathiepine bromhydrate (F 15845) prevents ischemia-induced heart remodeling by reduction of the intracellular Na+ overload. J Pharmacol Exp Ther. 2009 Sep;330(3):696-703. doi: 10.1124/jpet.109.153122. Epub 2009 Jun 10. PMID: 19515969.
6: Vacher B, Pignier C, Létienne R, Verscheure Y, Le Grand B. F 15845 inhibits persistent sodium current in the heart and prevents angina in animal models. Br J Pharmacol. 2009 Jan;156(2):214-25. doi: 10.1111/j.1476-5381.2008.00062.x. Epub 2009 Jan 7. PMID: 19133985; PMCID: PMC2697839.
7: Saint DA. Persistent (current) in the face of adversity ... a new class of cardiac anti-ischaemic compounds on the horizon? Br J Pharmacol. 2009 Jan;156(2):211-3. doi: 10.1111/j.1476-5381.2008.00077.x. Epub 2009 Jan 7. PMID: 19133984; PMCID: PMC2697828.