Synonym
EVP-6124; EVP6124; EVP 6124; MT-4666; MT4666; MT 4666; Encenicline
IUPAC/Chemical Name
N-[(3R)-1-Azabicyclo[2.2.2]octan-3-yl]-7-chloro-1-benzothiophene-2-carboxamide
InChi Key
SSRDSYXGYPJKRR-ZDUSSCGKSA-N
InChi Code
InChI=1S/C16H17ClN2OS/c17-12-3-1-2-11-8-14(21-15(11)12)16(20)18-13-9-19-6-4-10(13)5-7-19/h1-3,8,10,13H,4-7,9H2,(H,18,20)/t13-/m0/s1
SMILES Code
O=C(C1=CC2=CC=CC(Cl)=C2S1)N[C@H]3CN4CCC3CC4
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
320.84
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 |
1: Salaga M, Blomster LV, Piechota-Polańczyk A, Zielińska M, Jacenik D, Cygankiewicz AI, Krajewska WM, Mikkelsen JD, Fichna J. Encenicline, an α7 Nicotinic Acetylcholine Receptor Partial Agonist, Reduces Immune Cell Infiltration in the Colon and Improves Experimental Colitis in Mice. J Pharmacol Exp Ther. 2016 Jan;356(1):157-69. doi: 10.1124/jpet.115.228205. Epub 2015 Oct 13. PubMed PMID: 26462538.
2: Keefe RS, Meltzer HA, Dgetluck N, Gawryl M, Koenig G, Moebius HJ, Lombardo I, Hilt DC. Randomized, Double-Blind, Placebo-Controlled Study of Encenicline, an α7 Nicotinic Acetylcholine Receptor Agonist, as a Treatment for Cognitive Impairment in Schizophrenia. Neuropsychopharmacology. 2015 Dec;40(13):3053-60. doi: 10.1038/npp.2015.176. Epub 2015 Jun 19. PubMed PMID: 26089183; PubMed Central PMCID: PMC4864641.
3: Barbier AJ, Hilhorst M, Van Vliet A, Snyder P, Palfreyman MG, Gawryl M, Dgetluck N, Massaro M, Tiessen R, Timmerman W, Hilt DC. Pharmacodynamics, pharmacokinetics, safety, and tolerability of encenicline, a selective α7 nicotinic receptor partial agonist, in single ascending-dose and bioavailability studies. Clin Ther. 2015 Feb 1;37(2):311-24. doi: 10.1016/j.clinthera.2014.09.013. Epub 2014 Oct 14. PubMed PMID: 25438724.