2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 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.

For research use only. We do not sell to patients.

PF-03654764 Chemical Structure

PF-03654764 Chemical Structure

CAS No. : 935840-35-0

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Based on 1 publication(s) in Google Scholar

PF-03654764 Related Antibodies

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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].

IC50 & Target[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-03654764 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

350.45

Formula

C20H28F2N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1C[C@@](C2=CC(F)=C(CN3CCCC3)C=C2)(F)C1)NCC(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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PF-03654764 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-03654764935840-35-0PF03654764PF 03654764Histamine ReceptororallyH3FexofenadineallergicrhinitisInhibitorinhibitorinhibit

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