VU0486846

• CAT Number: I038162
• CAS Number: 1788055-11-7
• Molecular Formula: C25H28N4O3
• Molecular Weight: 432.51
• Purity: ≥95%
• IUPAC Name: (2R)-N-[(1S,2S)-2-hydroxycyclohexyl]-4-[(4-pyrazol-1-ylphenyl)methyl]-2,3-dihydro-1,4-benzoxazine-2-carboxamide
• InChI: InChI=1S/C25H28N4O3/c30-22-8-3-1-6-20(22)27-25(31)24-17-28(21-7-2-4-9-23(21)32-24)16-18-10-12-19(13-11-18)29-15-5-14-26-29/h2,4-5,7,9-15,20,22,24,30H,1,3,6,8,16-17H2,(H,27,31)/t20-,22-,24+/m0/s1
• SMILES: C1CC[C@@H]([C@H](C1)NC(=O)[C@H]2CN(C3=CC=CC=C3O2)CC4=CC=C(C=C4)N5C=CC=N5)O

VU0486846 is a potent and highly selective M1 PAM (EC50 value of 0.31 μM, 85%), devoid of agonist activity in the PFC, as well as cholinergic or other adverse effects in mice, rats and NHP, which results in robust procognitive activity in rodent models.
KEYWORDS: VU0486846 | supplier | M1 PAM | VU 0486846 | VU-0486846 | CAS [1788055-11-7] | Acetylcholine | CHRM1 | PAM | Receptors | Schizophrenia

Reference

JM Rook et al. A Novel M 1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity. ACS Chem Neurosci. 2018 Sep 19;9(9):2274-2285.