1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. PF-03654764

PF-03654764 

Cat. No.: HY-123812 Purity: >99.0%
Handling Instructions

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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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

Molecular Weight

350.45

Formula

C₂₀H₂₈F₂N₂O

CAS No.

935840-35-0

SMILES

O=C([[email protected]@H]1C[[email protected]@](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
References
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Keywords:

PF-03654764PF03654764PF 03654764Histamine ReceptororallyH3FexofenadineallergicrhinitisInhibitorinhibitorinhibit

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PF-03654764
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