PF-03654764

Modify Date: 2024-01-29 14:49:47

PF-03654764 structure	Common Name	PF-03654764
	CAS Number	935840-35-0	Molecular Weight	350.44600
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₀H₂₈F₂N₂O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of PF-03654764

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 allergic rhinitis research[1][2].

Name	3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutane-1-carboxamide
Synonym	More Synonyms

Description	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 allergic rhinitis research[1][2].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
Target	human 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)
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[1]. PF-03654764 has a human liver microsomes (HLM) T1/2 of 120 min and a HLM CLh <5 mL/min•kg[1].
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].
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. [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.

Molecular Formula	C₂₀H₂₈F₂N₂O
Molecular Weight	350.44600
Exact Mass	350.21700
PSA	35.83000
LogP	4.54670

unii-fpi2g03bj1

DC Chemicals Limited
China
Product Name: PF-03654764
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Purity: 98.0%
Stocking Period: 3 Day
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PF-03654764

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