PF-03654764

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PF-03654764 manufacturers

  • PF-03654764
  • PF-03654764 pictures
  • $328.00
  • 2026-05-11
  • CAS:935840-35-0
  • Purity: 100.00%
  • Supply Ability: 10g
PF-03654764 Basic information
Product Name:PF-03654764
Synonyms:PF-03654764;Cyclobutanecarboxamide, 3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]-N-(2-methylpropyl)-, trans-;3-Fluoro-3-(3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl)-N-(2-methylpropyl)cyclobutanecarboxamide
CAS:935840-35-0
MF:C20H28F2N2O
MW:350.45
EINECS:
Product Categories:
Mol File:935840-35-0.mol
PF-03654764 Structure
PF-03654764 Chemical Properties
Boiling point 478.1±45.0 °C(Predicted)
density 1.15±0.1 g/cm3(Predicted)
pka15.91±0.40(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
PF-03654764 Usage And Synthesis
UsesPF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research[1][2].
in vivo

PF-03654764 (10 mL/kg; oral; 14 days) has a Cmax of 8057 ng/mL and an AUC0-24 of 67400 ng h/mL in Sprague-Dawley rats[1].
PF-03654764 (1 mL/kg; oral; 7 days) has a Cmax of 6302 ng/mL and an AUC0-24 of 18175 ng h/mL in beagle dogs[1].

IC 50human H3 receptor: 1.2 nM (Ki); rat H3 receptor: 7.9 nM (Ki); human H3 receptor: 8.98 (pKi); rat H3 receptor: 8.10 (pKi)
References[1] Travis T Wager, et al. Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem. 2011 Nov 10;54(21):7602-20. DOI:10.1021/jm200939b
[2] Michelle L North, et al. Add-on histamine receptor-3 antagonist for allergic rhinitis: a double blind randomized crossover trial using the environmental exposure unit. Allergy Asthma Clin Immunol. 2014 Jul 3;10(1):33. DOI:10.1186/1710-1492-10-33
PF-03654764 Preparation Products And Raw materials
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