PF-03654764( PF 3654764 )

Catalog No. M16695 CAS No. 935840-35-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-03654764
Note

Research use only, not for human use.
Brief Description

PF-03654764 (PF 3654764) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 1.4 nM.
Description

PF-03654764 (PF 3654764) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 1.4 nM; displays >1000-fold selectivity versus H1, H2, H4 and other GPCRs (IC50>10 uM); possesses optimal pharmacological and pharmacokinetic profiles, shows potential in allergen-induced nasal symptoms. Allergy Phase 2 Discontinued.
In Vitro

PF-03654764 has pKi values of 8.98 and 8.10 for human H3 and rat H3 in whole cell assay, respectively. PF-03654764 has pKi values of 8.84, 7.73 and Ki values of 1.4 nM and 19 nM for human H3 and rat H3 in HEK-293 cells, respectively. PF-03654764 has >1000-fold selectivity for the H3 receptor over the other histamine receptor subtypes. PF-03654764 has a human liver microsomes (HLM) T1/2 of 120 min and a HLM CLh <5 mL/min?kg.
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. 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.
Synonyms

PF 3654764
Pathway

GPCR/G Protein
Target

Histamine Receptor
Recptor

Histamine Receptor
Research Area

Inflammation/Immunology
Indication

Allergy

CAS Number

935840-35-0
Formula Weight

322.454
Molecular Formula

C18H24F2N2O
Purity

>98% (HPLC)
Solubility

——
SMILES

CC(C)CNC(=O)C1CC(C1)(C2=CC(=C(C=C2)CN3CCCC3)F)F
Chemical Name

Trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide

1. Wager TT, et al. J Med Chem. 2011 Nov 10;54(21):7602-20. 2. North ML, et al. Allergy Asthma Clin Immunol. 2014 Jul 3;10(1):33.

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