PF-03654764

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-03654764 (PF 3654764) 是一种有效的、选择性的、口服生物活性的 H3 受体拮抗剂，Ki 为 1.4 nM。

PF-03654764 (PF 3654764) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 1.4 nM; displays >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.

PF-03654764 has pKi values of 8.98 and 8.10 for human H3 and rat H3 in whole cell assay, respectively. PF-03654764 has pKi values of 8.84, 7.73 and Ki values of 1.4 nM and 19 nM for human H3 and rat H3 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) T1/2 of 120 min and a HLM CLh <5 mL/min?kg.

PF-03654764 (10 mL/kg; oral; 14 days) has a Cmax of 8057 ng/mL and an AUC0-24 of 67400 ng?h/mL in Sprague-Dawley rats. PF-03654764 (1 mL/kg; oral; 7 days) has a Cmax of 6302 ng/mL and an AUC0-24 of 18175 ng?h/mL in beagle dogs.

PF 3654764

GPCR/G Protein

Histamine Receptor

Histamine Receptor

Inflammation/Immunology

Allergy

935840-35-0

322.454

C18H24F2N2O

>98% (HPLC)

——

CC(C)CNC(=O)C1CC(C1)(C2=CC(=C(C=C2)CN3CCCC3)F)F

Trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide

(-20℃)

With Ice Pack

≥ 2 years