MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 593084 | Name: AVE-2865

Description:

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

AVE-2865 is a biochemical.

Chemical Structure

AVE-2865
AVE-2865
CAS#648917-13-9

Theoretical Analysis

MedKoo Cat#: 593084

Name: AVE-2865

CAS#: 648917-13-9

Chemical Formula: C20H17ClF3N3O4

Exact Mass: 455.0860

Molecular Weight: 455.82

Elemental Analysis: C, 52.70; H, 3.76; Cl, 7.78; F, 12.50; N, 9.22; O, 14.04

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.
Bulk Inquiry
Related CAS #
No Data
Synonym
AVE-2865 AVE 2865; AVE2865
IUPAC/Chemical Name
1-(2-((((2-Chloro-4,5-difluorophenyl)carbonyl)carbamoyl)amino)-4-fluorophenyl)piperidine-4-carboxylic acid
InChi Key
KAJJGOCSAXKXBD-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H17ClF3N3O4/c21-13-9-15(24)14(23)8-12(13)18(28)26-20(31)25-16-7-11(22)1-2-17(16)27-5-3-10(4-6-27)19(29)30/h1-2,7-10H,3-6H2,(H,29,30)(H2,25,26,28,31)
SMILES Code
O=C(C1CCN(C2=CC=C(F)C=C2NC(NC(C3=CC(F)=C(F)C=C3Cl)=O)=O)CC1)O
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).
HS Tariff Code
2934.99.03.00
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 455.82 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: Kun A, Seprényi G, Varró A, Papp JG, Pataricza J. Neurogenic contraction induced by the antiarrhythmic compound, AVE 0118, in rat small mesenteric arteries. Basic Clin Pharmacol Toxicol. 2014 Oct;115(4):315-20. doi: 10.1111/bcpt.12225. Epub 2014 Apr 3. Erratum in: Basic Clin Pharmacol Toxicol. 2015 Apr;116(4):384. PubMed PMID: 24629214. 2: Tikhonov DB, Zhorov BS. Homology modeling of Kv1.5 channel block by cationic and electroneutral ligands. Biochim Biophys Acta. 2014 Mar;1838(3):978-87. doi: 10.1016/j.bbamem.2013.11.019. Epub 2013 Dec 5. PubMed PMID: 24316168. 3: Wirth KJ, Steinmeyer K, Ruetten H. Sensitization of upper airway mechanoreceptors as a new pharmacologic principle to treat obstructive sleep apnea: investigations with AVE0118 in anesthetized pigs. Sleep. 2013 May 1;36(5):699-708. doi: 10.5665/sleep.2630. PubMed PMID: 23633752; PubMed Central PMCID: PMC3624824. 4: Hillman D. A new pharmacological treatment to treat obstructive sleep apnea? Sleep. 2013 May 1;36(5):635-6. doi: 10.5665/sleep.2614. PubMed PMID: 23633744; PubMed Central PMCID: PMC3624816. 5: Burashnikov A, Barajas-Martinez H, Hu D, Nof E, Blazek J, Antzelevitch C. Atrial-selective prolongation of refractory period with AVE0118 is due principally to inhibition of sodium channel activity. J Cardiovasc Pharmacol. 2012 Jun;59(6):539-46. doi: 10.1097/FJC.0b013e31824e1b93. PubMed PMID: 22370957; PubMed Central PMCID: PMC3369013. 6: Bilodeau MT, Trotter BW. Kv1.5 blockers for the treatment of atrial fibrillation: approaches to optimization of potency and selectivity and translation to in vivo pharmacology. Curr Top Med Chem. 2009;9(5):436-51. Review. PubMed PMID: 19519460. 7: Schneider HJ, Husser O, Rihm M, Fredersdorf S, Birner C, Dhein S, Muders F, Jeron A, Goegelein H, Riegger GA, Luchner A. Safety of the novel atrial-selective K+-channel blocker AVE0118 in experimental heart failure. Naunyn Schmiedebergs Arch Pharmacol. 2009 Mar;379(3):225-32. doi: 10.1007/s00210-008-0361-0. Epub 2008 Oct 30. PubMed PMID: 18972103. 8: Christ T, Wettwer E, Voigt N, Hála O, Radicke S, Matschke K, Várro A, Dobrev D, Ravens U. Pathology-specific effects of the IKur/Ito/IK,ACh blocker AVE0118 on ion channels in human chronic atrial fibrillation. Br J Pharmacol. 2008 Aug;154(8):1619-30. doi: 10.1038/bjp.2008.209. Epub 2008 Jun 9. PubMed PMID: 18536759; PubMed Central PMCID: PMC2518460. 9: Billman GE, Kukielka M. Novel transient outward and ultra-rapid delayed rectifier current antagonist, AVE0118, protects against ventricular fibrillation induced by myocardial ischemia. J Cardiovasc Pharmacol. 2008 Apr;51(4):352-8. doi: 10.1097/FJC.0b013e31816586bd. PubMed PMID: 18427277. 10: Hernández GP, Ortíz PL, López FA, Mondragón Ldel V. [New antiarrhythmic agents in atrial fibrillation]. Arch Cardiol Mex. 2007 Apr-Jun;77 Suppl 2:S2-59-S2-63. Review. Spanish. PubMed PMID: 17972381. 11: London B. Amiodarone and atrial fibrillation. J Cardiovasc Electrophysiol. 2007 Dec;18(12):1321-2. Epub 2007 Oct 24. PubMed PMID: 17971150. 12: Linz DK, Afkham F, Itter G, Rütten H, Wirth KJ. Effect of atrial electrical remodeling on the efficacy of antiarrhythmic drugs: comparison of amiodarone with I(Kr)- and I(to)/IKur-blockade in vivo. J Cardiovasc Electrophysiol. 2007 Dec;18(12):1313-20. Epub 2007 Oct 4. PubMed PMID: 17916155. 13: Naccarelli GV, Wolbrette DL, Samii S, Banchs JE, Penny-Peterson E, Gonzalez MD. New antiarrhythmic treatment of atrial fibrillation. Expert Rev Cardiovasc Ther. 2007 Jul;5(4):707-14. Review. PubMed PMID: 17605649. 14: Blaauw Y, Schotten U, van Hunnik A, Neuberger HR, Allessie MA. Cardioversion of persistent atrial fibrillation by a combination of atrial specific and non-specific class III drugs in the goat. Cardiovasc Res. 2007 Jul 1;75(1):89-98. Epub 2007 Mar 30. Erratum in: Cardiovasc Res. 2007 Nov 1;76(2):373. Dosage error in published abstract; MEDLINE/PubMed abstract corrected. PubMed PMID: 17466958. 15: Schotten U, de Haan S, Verheule S, Harks EG, Frechen D, Bodewig E, Greiser M, Ram R, Maessen J, Kelm M, Allessie M, Van Wagoner DR. Blockade of atrial-specific K+-currents increases atrial but not ventricular contractility by enhancing reverse mode Na+/Ca2+-exchange. Cardiovasc Res. 2007 Jan 1;73(1):37-47. Epub 2006 Nov 23. PubMed PMID: 17157284. 16: Oros A, Volders PG, Beekman JD, van der Nagel T, Vos MA. Atrial-specific drug AVE0118 is free of torsades de pointes in anesthetized dogs with chronic complete atrioventricular block. Heart Rhythm. 2006 Nov;3(11):1339-45. Epub 2006 Jul 20. PubMed PMID: 17074641. 17: de Haan S, Greiser M, Harks E, Blaauw Y, van Hunnik A, Verheule S, Allessie M, Schotten U. AVE0118, blocker of the transient outward current (I(to)) and ultrarapid delayed rectifier current (I(Kur)), fully restores atrial contractility after cardioversion of atrial fibrillation in the goat. Circulation. 2006 Sep 19;114(12):1234-42. Epub 2006 Aug 28. PubMed PMID: 16940189. 18: Decher N, Kumar P, Gonzalez T, Pirard B, Sanguinetti MC. Binding site of a novel Kv1.5 blocker: a "foot in the door" against atrial fibrillation. Mol Pharmacol. 2006 Oct;70(4):1204-11. Epub 2006 Jul 11. PubMed PMID: 16835355. 19: Löfberg L, Jacobson I, Carlsson L. Electrophysiological and antiarrhythmic effects of the novel antiarrhythmic agent AZD7009: a comparison with azimilide and AVE0118 in the acutely dilated right atrium of the rabbit in vitro. Europace. 2006 Jul;8(7):549-57. PubMed PMID: 16798770. 20: Wettwer E, Hála O, Christ T, Heubach JF, Dobrev D, Knaut M, Varró A, Ravens U. Role of IKur in controlling action potential shape and contractility in the human atrium: influence of chronic atrial fibrillation. Circulation. 2004 Oct 19;110(16):2299-306. Epub 2004 Oct 11. PubMed PMID: 15477405.

View History

AVE-5997 mesylate

AVE-5997 mesylate