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PF-03654746

Chemical Structure : PF-03654746

CAS No.: 935840-31-6

PF-03654746 (PF 3654746)

Catalog No.: PC-63034Not For Human Use, Lab Use Only.

PF-03654746 (PF 3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PF-03654746 (PF 3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 nM; dislaplays >1000-fold selectivity versus H1, H2, H4 and other GPCRs (IC50>10 uM); possesses optimal pharmacological and pharmacokinetic profiles, shows potential in allergen-induced nasal symptoms.

Allergy

Phase 2 Discontinued

Physicochemical Properties

M.Wt 322.4
Formula C18H24F2N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide

References

1. Wager TT, et al. J Med Chem. 2011 Nov 10;54(21):7602-20.

2. Stokes JR, et al. J Allergy Clin Immunol. 2012 Feb;129(2):409-12, 412.e1-2.

3. Gallezot JD, et al. J Cereb Blood Flow Metab. 2017 Mar;37(3):1095-1107.

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