PF-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 al
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Shipped In
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Action Type
ANTAGONIST
Mechanism of action
Histamine H3 receptor antagonist
Product Description
PF-03654764 has pK i values of 8.98 and 8.10 for human H 3 and rat H 3 in whole cell assay, respectively. PF-03654764 has pK i values of 8.84, 7.73 and K i values of 1.4 nM and 19 nM for human H 3 and rat H 3 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) T 1/2 of 120 min and a HLM CL h <5 mL/min•kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PF-03654764 (10 mL/kg; oral; 14 days) has a C max of 8057 ng/mL and an AUC 0-24 of 67400 ng•h/mL in Sprague-Dawley rats . PF-03654764 (1 mL/kg; oral; 7 days) has a C max of 6302 ng/mL and an AUC 0-24 of 18175 ng•h/mL in beagle dogs . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:human H 3 receptor 1.2 nM (Ki) rat H 3 receptor 7.9 nM (Ki) human H 3 receptor 8.98 (pKi) rat H 3 receptor 8.10 (pKi)
This compound belongs to the class of organic compounds known as phenylmethylamines. These are compounds containing a phenylmethtylamine moiety, which consists of a phenyl group substituted by an methanamine.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
