VU0357017 (hydrochloride)

VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs, Ki = 9.91 µM in CHO cells). In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors. In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.Formal Name: 4-[[2-[(2-methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid, ethyl ester, monohydrochloride. CAS Number: 1135242-13-5. Synonyms: CID-25010775. Molecular Formula: C18H27N3O3 . HCl. Formula Weight: 369.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 3 mg/ml, PBS (pH 7.2): 5 mg/ml. SMILES: CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl. InChi Code: InChI=1S/C18H27N3O3.ClH/c1-3-24-18(23)21-12-8-15(9-13-21)19-10-11-20-17(22)16-7-5-4-6-14(16)2,/h4-7,15,19H,3,8-13H2,1-2H3,(H,20,22),1H. InChi Key: XKJQVUIXSBOCPP-UHFFFAOYSA-N.