PF-06767832

Name: PF-06767832
CAS#: 1859081-58-5
Chemical Formula: C22H23N3O3S
Exact Mass: 409.146
Molecular Weight: 409.504
Elemental Analysis: C, 64.53; H, 5.66; N, 10.26; O, 11.72; S, 7.83

Description: PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling suggested that despite being devoid of mAChR M2/M3 subtype activity, compound 38 still carries gastrointestinal and cardiovascular side effects. These data provide strong evidence that M1 activation contributes to the cholinergic liabilities that were previously attributed to activation of the M2 and M3 receptors.

IUPAC/Chemical Name: N-((3R,4S)-3-hydroxytetrahydro-2H-pyran-4-yl)-5-methyl-4-(4-(thiazol-4-yl)benzyl)picolinamide

InChi Key: VVZZHFMLRHJXTO-RXVVDRJESA-N

InChi Code: InChI=1S/C22H23N3O3S/c1-14-10-23-19(22(27)25-18-6-7-28-11-21(18)26)9-17(14)8-15-2-4-16(5-3-15)20-12-29-13-24-20/h2-5,9-10,12-13,18,21,26H,6-8,11H2,1H3,(H,25,27)/t18-,21-/m0/s1

SMILES Code: O=C(C1=NC=C(C)C(CC2=CC=C(C3=CSC=N3)C=C2)=C1)N[C@@H]4[C@@H](O)COCC4

Appearance: Solid powder