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PF-03654764

Catalog No. T61213 CAS 935840-35-0

PF-03654764 is an orally active, potent, and selective histamine H3 receptor antagonist that inhibits human H3 and rat H3 with Ki values of 1.2 nM and 7.9 nM, respectively.PF-03654764 is often co-administered with Fexofenadine for the treatment of allergic rhinitis.

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PF-03654764, CAS 935840-35-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 328.00
5 mg	In stock	$ 789.00
10 mg	In stock	$ 1,070.00
25 mg	6-8 weeks	$ 1,590.00
50 mg	6-8 weeks	$ 2,150.00

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Purity: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-03654764 is an orally active, potent, and selective histamine H3 receptor antagonist that inhibits human H3 and rat H3 with Ki values of 1.2 nM and 7.9 nM, respectively.PF-03654764 is often co-administered with Fexofenadine for the treatment of allergic rhinitis.
Targets&IC50	H3 receptor:8.10 (pKi,rat), H3 receptor:1.2 nM (Ki) (human), H3 receptor:8.98 (pKi,human), H3 receptor:7.9 nM (Ki,rat )
In vitro	In a whole cell assay, PF-03654764 exhibits pKi values of 8.98 and 8.10 for human H3 and rat H3, respectively. In HEK-293 cells, PF-03654764 demonstrates pKi values of 8.84 and 7.73, as well as Ki values of 1.4 nM and 19 nM for human H3 and rat H3, respectively. Notably, PF-03654764 displays >1000-fold selectivity for the H3 receptor over the other histamine receptor subtypes[1].Regarding its pharmacokinetics, PF-03654764 has a half-life (T1/2) of 120 minutes in human liver microsomes (HLM) and a clearance (CLh) of less than 5 mL/min•kg in HLM[2].
In vivo	In Sprague-Dawley rats, PF-03654764 administered orally at a dose of 10 mL/kg for 14 days results in a Cmax of 8057 ng/mL and an AUC0-24 of 67400 ng•h/mL[2]. Similarly, in beagle dogs, oral administration of PF-03654764 at a dose of 1 mL/kg for 7 days yields a Cmax of 6302 ng/mL and an AUC0-24 of 18175 ng•h/mL[2].

Molecular Weight	350.45
Formula	C20H28F2N2O
CAS No.	935840-35-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. 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. 2. Wager TT,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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library

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Keywords

PF-03654764 935840-35-0 Immunology/Inflammation Neuroscience GPCR/G Protein Histamine Receptor inhibitor inhibit

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