EVP-6124 (hydrochloride)

EVP-6124 is a partial agonist of alpha7 subunit-containing nicotinic acetylcholine receptors (nAChRs, IC50 = 22.38 nM). It is 1,000-fold selective for alpha7 subunit-containing nAChRs over alpha4beta2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human alpha7 subunit-containing nAChRs (EC50 = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).Formal Name: N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-7-chloro-benzo[b]thiophene-2-carboxamide, monohydrochloride. CAS Number: 550999-74-1. Molecular Formula: C16H17ClN2OS . HCl. Formula Weight: 357.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml, Ethanol: 20 mg/ml. lambdamax: 244, 281 nm. SMILES: ClC1=C2C(C=C(C(N[C@@H]3C4CCN(CC4)C3)=O)S2)=CC=C1.Cl. InChi Code: InChI=1S/C16H17ClN2OS.ClH/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),1H/t13-,/m0./s1. InChi Key: OIJYTJGIDVTCFF-ZOWNYOTGSA-N.