PF-03654746 (Tosylate)

• UNSPSC Description:

  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].

• Target Antigen:

  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:

  H2O : 8.4 mg/mL (ultrasonic;warming)|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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  Phase 2

• CAS Number:

  1039399-17-1