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PF0346275

Names

[ CAS No. ]:
1173239-39-8

[ Name ]:
PF0346275

[Synonym ]:
N-(3-Chloro-4-fluorobenzyl)-1-methyl-N-{[(1R,5S,6r)-3-methyl-3-azabicyclo[3.1.0]hex-6-yl]methyl}-1H-imidazole-4-carboxamide dihydrochloride
1H-Imidazole-4-carboxamide, N-[(3-chloro-4-fluorophenyl)methyl]-1-methyl-N-[[(1R,5S)-3-methyl-3-azabicyclo[3.1.0]hex-6-yl]methyl]-, hydrochloride (1:2)

Biological Activity

[Description]:

A potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM); demonstrates potent activity in elevating CSF levels of glycine in vivo (ED200, 3.5 mg/kg).

[References]

References 1. Lowe JA 3rd, et al. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2974-6. 2. Yamamoto S, et al. Chem Pharm Bull (Tokyo). 2016;64(11):1630-1640. View Related Products by Target Glycine Transporter (GlyT)

Chemical & Physical Properties

[ Molecular Formula ]:
C19H22ClFN4O

[ Molecular Weight ]:
449.777

[ Exact Mass ]:
448.099976


Related Compounds