VU 0357017 Hydrochloride

CAS: 1135242-13-5

Ref. TR-V787500

Product Information

• Name: VU 0357017 Hydrochloride
• Synonyms: 4-[[2-[(2-Methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic Acid Ethyl Ester Hydrochloride

Description

Applications VU0357017 is a subtype-selective M1 muscarinic acetylcholine allosteric agonist. VU0357017 has a potency of 200 nM and Achmax of 81% and had no activity at M2-M5 up to the highest concentrations tested and also had little or no detectable antagonist activity at any other mAChR subtype at concentrations over 2 orders of magnitude higher than those required to activate M1 or activity at a large panel of GPCRs, ion channels, and transporters. In contrast, TBPB inhibited responses to ACh at each of the other mAChR subtypes. VU0357017 was active in reversing cognitive deficits induced by Scopolamine (S200000) in a preclinical rodent model.
References Bridges, et al.: Bioorg. Med. Chem. Lett., 20, 1972 (2010); Lebois, et al.: ACS Chem. Neurosci., 1, 104 (2010),

• Brand: TRC

Chemical properties

• Molecular weight: 369.886
• Formula: C₁₈H₂₇N₃O₃·ClH
• Color/Form: Neat
• InChI: 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: InChIKey=XKJQVUIXSBOCPP-UHFFFAOYSA-N
• SMILES: CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1.Cl