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EVP-6124 hydrochloride

Cat. No. M7227
EVP-6124 hydrochloride Structure

Encenicline hydrochloride

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5mg USD 288  USD320 In stock
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Biological Activity

EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs). Encenicline hydrochloride inhibits the 5-HT3 receptor by 51% at 10 nM, the lowest concentration tested. Evaluation of the human 5-HT2B receptor expressed in CHO cells demonstrates displacement of [3H]-mesulergine (Ki=14 nM) and only antagonist activity in the rat gastric fundus assay at an IC50 of 16 μM. In binding and functional experiments, Encenicline (EVP-6124) shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 357.30
Formula C16H18Cl2N2OS
CAS Number 550999-74-1
Purity 99.98%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C

EVP-6124, a Novel and Selective α7 Nicotinic Acetylcholine Receptor Partial Agonist, Improves Memory Performance by Potentiating the Acetylcholine Response of α7 Nicotinic Acetylcholine Receptors
Jos Prickaerts, et al. Neuropharmacology. 2012 Feb;62(2):1099-110. PMID: 22085888.

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Keywords: EVP-6124 hydrochloride, Encenicline hydrochloride supplier, AChR/AChE, inhibitors

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