PF-03654764 has pK i values of 8.98 and 8.10 for human H 3 and rat H 3 in whole cell assay, respectively. PF-03654764 has pK i values of 8.84, 7.73 and K i values of 1.4 nM and 19 nM for human H 3 and rat H 3 in HEK-293 cells, respectively. PF-03654764 has >1000-fold selectivity for the H3 receptor over the other histamine receptor subtypes. PF-03654764 has a human liver microsomes (HLM) T 1/2 of 120 min and a HLM CL h In Vivo PF-03654764 (10 mL/kg; oral; 14 days) has a C max of 8057 ng/mL and an AUC 0-24 of 67400 ng•h/mL in Sprague-Dawley rats . PF-03654764 (1 mL/kg; oral; 7 days) has a C max of 6302 ng/mL and an AUC 0-24 of 18175 ng•h/mL in beagle dogs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:human H 3 receptor 1.2 nM (Ki) rat H 3 receptor 7.9 nM (Ki) human H 3 receptor 8.98 (pKi) rat H 3 receptor 8.10 (pKi)
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PF-03654764
CAS number：935840-35-0 molecular formula：C20H28F2N2O
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | H3 receptor antagonist 1 | Cyclobutanecarboxamide, 3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]-N-(2-methylpropyl)-, trans- | ||
| CAS number | 935840-35-0 | molecular formula | C20H28F2N2O |
| molecular weight | 350.45 g/mol | Exact mass | ≥98% |
| PSA | 32.299 Ų | logp | 3.400 |
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