Basic information Safety Supplier Related

PF 03463275

Basic information Safety Supplier Related

PF 03463275 Basic information

Product Name:
PF 03463275
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]-
  • PF-03463275, 10 mM in DMSO
  • 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]-
CAS:
1173239-39-8
MF:
C19H22ClFN4O
MW:
376.86
Mol File:
1173239-39-8.mol
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PF 03463275 Chemical Properties

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)
pka
10.07±0.40(Predicted)
form 
Solid
color 
Off-white to light yellow
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PF 03463275 Usage And Synthesis

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.

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

PF 03463275Supplier

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