| Identification | Back Directory | [Name]
PF 03463275 | [CAS]
1173239-39-8 | [Synonyms]
PF0346275
1H-Imidazole-4-carboxamide, N-[(3-chloro-4-fluorophenyl)methyl]-1-methyl-N-[[(1α,5α,6α)-3-methyl-3-azabicyclo[3.1.0]hex-6-yl]methyl]- | [Molecular Formula]
C19H22ClFN4O | [MOL File]
1173239-39-8.mol | [Molecular Weight]
376.86 |
| Chemical Properties | Back Directory | [Melting point ]
125 °C | [Boiling point ]
575.8±45.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 33.33 mg/mL (88.44 mM) | [form ]
Solid | [pka]
10.07±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research[1][2]. | [in vivo]
PF-03463275 (1-10 mg/kg; s.c.) attenuates oscillatory potentials (OPs)[2]. | Animal Model: | Male Sprague-Dawley rats[2] | | Dosage: | 1, 3 and 10 mg/kg | | Administration: | S.c. | | Result: | A dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from the dark-adapted rats.
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| [IC 50]
GlyT1 | [References]
[1] Lowe JA 3rd, et al. The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter [published correction appears in Bioorg Med Chem Lett. 2009 Aug 15;19(16):4885. Bronk, Brian S [added]; Schaeffer, Eric [added]]. Bioorg Med Chem Lett. 2009;19(11):2974-2976. DOI:10.1016/j.bmcl.2009.04.035
[2] Liu CN, Pettersen B, Seitis G, Osgood S, Somps C. GlyT1 inhibitor reduces oscillatory potentials of the electroretinogram in rats. Cutan Ocul Toxicol. 2014;33(3):206-211. DOI:10.3109/15569527.2013.833937 |
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| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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