PF-06827443

Names

[ Name ]:
PF-06827443

[Synonym ]:
2-((3R,4S)-3-Hydroxytetrahydro-pyran-4-yl)-5-methyl-6-(4-oxazol-4-yl-benzyl)-2,3-dihydro-isoindol-1-one
PF-06827443
L-threo-Pentitol, 1,5-anhydro-2,3-dideoxy-3-[1,3-dihydro-5-methyl-6-[[4-(4-oxazolyl)phenyl]methyl]-1-oxo-2H-isoindol-2-yl]-
1,5-Anhydro-2,3-dideoxy-3-{5-methyl-6-[4-(1,3-oxazol-4-yl)benzyl]-1-oxo-1,3-dihydro-2H-isoindol-2-yl}-L-threo-pentitol

Biological Activity

[Description]:

PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM; induces cholinergic adverse events and convulsion at therapeutic indices similar to previous compounds with more agonist activity.

[References]

References 1. Davoren JE, et al. J Med Chem. 2017 Aug 10;60(15):6649-6663. 2. Moran SP, et al. ACS Chem Neurosci. 2018 Apr 25. doi: 10.1021/acschemneuro.8b00106. View Related Products by Target mAChR

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
669.7±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₄N₂O₄

[ Molecular Weight ]:
404.458

[ Flash Point ]:
358.8±31.5 °C

[ Exact Mass ]:
404.173615

[ LogP ]:
1.79

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.631

Related Compounds

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