MG624

MG624 is an antagonist of neuronal nicotinic acetylcholine receptors (nAChRs, Ki = 0.055 µM in neuronal chick optic lobe membranes). It is selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM in TE671 cells that express muscle-type AChRs). MG624 inhibits currents evoked by acetylcholine in Xenopus oocytes expressing chick alpha7 subunit-containing nAChRs (IC50 = 94 nM). It is selective for alpha7 subunit-containing nAChRs over alpha6, beta2, and beta4 subunit-containing nAChRs (Kis = 4.52, 12, and 9.2 µM, respectively). It selectively decreases vagus nerve stimulation-induced contractions of isolated guinea pig vagus nerve-stomach preparations (EC50 = 49.4 µM) over isolated rat phrenic nerve-hemidiaphragm preparations (EC50 = 486 µM). MG624 decreases protein levels of early growth response gene 1 (Egr-1) induced by nicotine in human microvascular endothelial cells of the lung (HMEC-Ls). It also decreases proliferation of HMEC-Ls and inhibits angiogenesis in vitro and ex vivo as well as in an H69 small cell lung cancer (SCLC) mouse xenograft model concomitant with a reduction in tumor growth when administered in the diet at a dose of approximately 10 mg/kg per day.Formal Name: N,N,N-triethyl-2-[4-[(1E)-2-phenylethenyl]phenoxy]-ethanaminium, monoiodide. CAS Number: 77257-42-2. Molecular Formula: C22H30NO . I. Formula Weight: 451.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mM, PBS (pH 7.2): 0.3 mg/ml. lambdamax: 204, 224, 302 nm. SMILES: CC[N+](CC)(CC)CCOC(C=C1)=CC=C1/C=C/C2=CC=CC=C2.[I-]. InChi Code: InChI=1S/C22H30NO.HI/c1-4-23(5-2,6-3)18-19-24-22-16-14-21(15-17-22)13-12-20-10-8-7-9-11-20,/h7-17H,4-6,18-19H2,1-3H3,1H/q+1,/p-1/b13-12+,. InChi Key: RDTKUZXIHMTSJO-UEIGIMKUSA-M.