PF-03654746 (Tosylate)

PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms[1]. PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) [2].

Product Specifications

CAS Number

[1039399-17-1]

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Endocrinology; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pf-03654746-tosylate.html

Purity

99.65

Solubility

10 mM in DMSO

Smiles

O=C([C@H]1C[C@](C1)(F)C2=CC=C(CN3CCCC3)C(F)=C2)NCC.O=S(C4=CC=C(C)C=C4)(O)=O

Molecular Formula

C25H32F2N2O4S

Molecular Weight

494.59

References & Citations

[1]Stokes JR, et al. The effects of an H3 receptor antagonist (PF-03654746) with fexofenadine on reducing allergic rhinitis symptoms. J Allergy Clin Immunol. 2012 Feb;129 (2) :409-12, 412.e1-2.|[2]Brioni JD, et al. Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease. J Pharmacol Exp Ther. 2011 Jan;336 (1) :38-46.|[3]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.