L-768673

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

MedKoo CAT#: 563613

CAS#: 177954-68-6

Description: L-768673 is a class III antiarrhythmic agent, selectively blocking the slowly activating cardiac delayed rectifier potassium current Iks.


Price and Availability

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L-768673 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.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 563613
Name: L-768673
CAS#: 177954-68-6
Chemical Formula: C27H18F9N3O2
Exact Mass: 587.1255
Molecular Weight: 587.44
Elemental Analysis: C, 55.20; H, 3.09; F, 29.11; N, 7.15; O, 5.45


Synonym: L-768673; L 768673; L768673;

IUPAC/Chemical Name: 2-[2,4-Bis(trifluoromethyl)phenyl]-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]acetamide

InChi Key: VVCYJFVTVHMTBV-HSZRJFAPSA-N

InChi Code: InChI=1S/C27H18F9N3O2/c28-25(29,30)14-39-20-9-5-4-8-18(20)22(15-6-2-1-3-7-15)38-23(24(39)41)37-21(40)12-16-10-11-17(26(31,32)33)13-19(16)27(34,35)36/h1-11,13,23H,12,14H2,(H,37,40)/t23-/m1/s1

SMILES Code: O=C(N[C@H]1C(N(CC(F)(F)F)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)CC4=CC=C(C(F)(F)F)C=C4C(F)(F)F


Technical Data

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:
>3 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).

Harmonized System Code:
2934.99.03.00


References

1: Guo X, Gao X, Wang Y, Peng L, Zhu Y, Wang S. IKs protects from ventricular arrhythmia during cardiac ischemia and reperfusion in rabbits by preserving the repolarization reserve. PLoS One. 2012;7(2):e31545. doi: 10.1371/journal.pone.0031545. Epub 2012 Feb 22. PubMed PMID: 22384037; PubMed Central PMCID: PMC3285162.

2: Taniguchi T, Uesugi M, Arai T, Yoshinaga T, Miyamoto N, Sawada K. Chronic probucol treatment decreases the slow component of the delayed-rectifier potassium current in CHO cells transfected with KCNQ1 and KCNE1: a novel mechanism of QT prolongation. J Cardiovasc Pharmacol. 2012 Apr;59(4):377-86. doi: 10.1097/FJC.0b013e318245e0c5. PubMed PMID: 22189896.

3: Fossa AA, Wisialowski T, Crimin K. QT prolongation modifies dynamic restitution and hysteresis of the beat-to-beat QT-TQ interval relationship during normal sinus rhythm under varying states of repolarization. J Pharmacol Exp Ther. 2006 Feb;316(2):498-506. Epub 2005 Oct 4. PubMed PMID: 16204470.

4: Salataa JJ, Selnickb HG, Lynch JJ Jr. Pharmacological modulation of I(Ks): potential for antiarrhythmic therapy. Curr Med Chem. 2004 Jan;11(1):29-44. Review. PubMed PMID: 14754424.

5: Stump GL, Smith GR, Tebben AJ, Jahansouz H, Salata JJ, Selnick HG, Claremon DA, Lynch JJ Jr. In vivo canine cardiac electrophysiologic profile of 1,4-benzodiazepine IKs blockers. J Cardiovasc Pharmacol. 2003 Jul;42(1):105-12. PubMed PMID: 12827034.

6: Lynch JJ Jr, Salata JJ, Wallace AA, Stump GL, Gilberto DB, Jahansouz H, Liverton NJ, Selnick HG, Claremon DA. Antiarrhythmic efficacy of combined I(Ks) and beta-adrenergic receptor blockade. J Pharmacol Exp Ther. 2002 Jul;302(1):283-9. PubMed PMID: 12065728.

7: Han W, Wang Z, Nattel S. Slow delayed rectifier current and repolarization in canine cardiac Purkinje cells. Am J Physiol Heart Circ Physiol. 2001 Mar;280(3):H1075-80. PubMed PMID: 11179049.

8: Whitworth CA, Rybak LP, Kemp R, Spence S. Pharmacological antagonism of the slow-activating delayed rectifying potassium channel (I(Ks)) has no effect on cochlear structure and function in vivo. Pharmacol Toxicol. 2001 Jan;88(1):45-50. PubMed PMID: 11169161.

9: Lynch JJ Jr, Houle MS, Stump GL, Wallace AA, Gilberto DB, Jahansouz H, Smith GR, Tebben AJ, Liverton NJ, Selnick HG, Claremon DA, Billman GE. Antiarrhythmic efficacy of selective blockade of the cardiac slowly activating delayed rectifier current, I(Ks), in canine models of malignant ischemic ventricular arrhythmia. Circulation. 1999 Nov 2;100(18):1917-22. PubMed PMID: 10545437.

10: Spence S, Soper K, Hoe CM, Coleman J. The heart rate-corrected QT interval of conscious beagle dogs: a formula based on analysis of covariance. Toxicol Sci. 1998 Oct;45(2):247-58. PubMed PMID: 9848132.

11: Kenney RR, Forsyth RJ, Jahansouz H. Solid-phase extraction and liquid chromatographic quantitation of the antiarrhythmic drug L-768673 in a microemulsion formulation. J Pharm Biomed Anal. 1998 Aug;17(4-5):679-87. PubMed PMID: 9682151.

12: Selnick HG, Liverton NJ, Baldwin JJ, Butcher JW, Claremon DA, Elliott JM, Freidinger RM, King SA, Libby BE, McIntyre CJ, Pribush DA, Remy DC, Smith GR, Tebben AJ, Jurkiewicz NK, Lynch JJ, Salata JJ, Sanguinetti MC, Siegl PK, Slaughter DE, Vyas K. Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide. J Med Chem. 1997 Nov 21;40(24):3865-8. PubMed PMID: 9397166.