Product data sheet MedKoo Cat#: 510298 Name: HCl salt CAS#: 550999-74-1 (HCl) Chemical Formula: C16H18Cl2N2OS Exact Mass: 356.0517 Molecular Weight: 357.3 Product supplied as: Powder Purity (by HPLC): ≥ 98% Shipping conditions Ambient temperature Storage conditions: Powder: -20°C 3 years; 4°C 2 years. In solvent: -80°C 3 months; -20°C 2 weeks.

1. Product description: Encenicline, also known as EVP-6124 and MT-4666, is a novel α7 nicotinic receptor that enhances , acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens. EVP-6124 improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors.

2. CoA, QC data, SDS, and handling instruction SDS and handling instruction, CoA with copies of QC data (NMR, HPLC and MS analytical spectra) can be downloaded from the product web page under “QC And Documents” section. Note: copies of analytical spectra may not be available if the product is being supplied by MedKoo partners. Whether the product was made by MedKoo or provided by its partners, the quality is 100% guaranteed.

3. Solubility data Solvent Max Conc. mg/mL Max Conc. mM DMSO 40.0 111.95 DMSO:PBS (pH 7.2) 0.16 0.45 (1.5) DMF 30.0 83.96 Ethanol 20.0 55.98

4. Stock solution preparation table: Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg 1 mM 2.80 mL 13.99 mL 27.99 mL 5 mM 0.56 mL 2.80 mL 5.60 mL 10 mM 0.28 mL 1.40 mL 2.80 mL 50 mM 0.06 mL 0.28 mL 0.56 mL

5. Molarity Calculator, Reconstitution Calculator, Dilution Calculator Please refer the product web page under section of “Calculator”

6. Recommended literature which reported protocols for in vitro and in vivo study In vitro study 1. Prickaerts J, van Goethem NP, Chesworth R, Shapiro G, Boess FG, Methfessel C, Reneerkens OA, Flood DG, Hilt D, Gawryl M, Bertrand S, Bertrand D, König G. EVP-6124, a novel and selective α7 nicotinic partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. Neuropharmacology. 2012 Feb;62(2):1099-110. doi: 10.1016/j.neuropharm.2011.10.024. Epub 2011 Nov 10. PMID: 22085888.

In vivo study 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. PMID: 26462538.

MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831

Product data sheet 2. Hayward A, Adamson L, Neill JC. Partial agonism at the α7 nicotinic acetylcholine receptor improves attention, impulsive action and vigilance in low attentive rats. Eur Neuropsychopharmacol. 2017 Apr;27(4):325-335. doi: 10.1016/j.euroneuro.2017.01.013. Epub 2017 Feb 1. PMID: 28161246.

7. Bioactivity Biological target: Encenicline hydrochloride (EVP-6124 hydrochloride) is a partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

In vitro activity EVP-6124, (R)-7-chloro-N-quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs) that was evaluated here in vitro and in vivo. In binding and functional experiments, EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.

Reference: Neuropharmacology. 2012 Feb;62(2):1099-110. https://pubmed.ncbi.nlm.nih.gov/22085888/

In vivo activity Treatment with encenicline significantly reduced the infiltration of macrophages, neutrophils, and B cells in the colon of TNBS- treated animals, as indicated by IHC. In the TNBS model encenicline reduced the frequency of FoxP3(+) IL-17A(+) T cells in the colon. In the DSS-model treatment encenicline increased the frequency of FoxP3(+) T cells and reduced IL-17A(+) T cells. Stimulation of α7 nAChR with partial agonist encenicline alleviates colitis via alteration of the number and/or activation status of the immune cells in the gut, emphasizing a potential role of α7 nAChRs as a target for anticolitic drugs.

Reference: J Pharmacol Exp Ther. 2016 Jan;356(1):157-69. https://pubmed.ncbi.nlm.nih.gov/26462538/

Note: The information listed here was extracted from literature. MedKoo has not independently retested and confirmed the accuracy of these methods. Customer should use it just for a reference only.

MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831