PF-03654764 binds with high affinity to the human H3 receptor and with lower affinity to the rat H3 receptor, in addition to having >1000-fold selectivity versus other human histamine receptor subtypes (H1, H2, and H4). PF-03654764 displayed potent antagonist properties in functional assays measuring cAMP utilizing a reporter gene assay (β-lactamase) in HEK293 cells stably expressing full length human or rat H3 receptors.
MedKoo Cat#: 125727
Name: PF-03654764 tosylate
CAS#: 1337536-85-2 (tosylate)
Chemical Formula: C27H36F2N2O4S
Exact Mass: 522.2400
Molecular Weight: 522.65
Elemental Analysis: C, 62.05; H, 6.94; F, 7.27; N, 5.36; O, 12.24; S, 6.13
The following data is based on the product molecular weight 522.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |