PF-03654746 Tosylate

• CAT Number: I046127
• CAS Number: 1039399-17-1
• Molecular Formula: C25H32F2N2O4S
• Molecular Weight: 494.59
• Purity: ≥95%
• Synonyms: N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide;4-methylbenzenesulfonic acid
• InChI: InChI=1S/C18H24F2N2O.C7H8O3S/c1-2-21-17(23)14-10-18(20,11-14)15-6-5-13(16(19)9-15)12-22-7-3-4-8-22;1-6-2-4-7(5-3-6)11(8,9)10/h5-6,9,14H,2-4,7-8,10-12H2,1H3,(H,21,23);2-5H,1H3,(H,8,9,10)
• InChIKey: IKAYTZLLIWAEDV-UHFFFAOYSA-N
• SMILES: CCNC(=O)C1CC(C1)(C2=CC(=C(C=C2)CN3CCCC3)F)F.CC1=CC=C(C=C1)S(=O)(=O)O

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].

Reference

[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.
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[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.
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[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-meth
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