PF-03654764|935840-35-0|-陌孚医药/Medlife

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PF-03654764

目录号: PL09464 纯度: ≥99.0%

CAS No. :935840-35-0

商品编号	规格	价格	会员价
PL09464-1mg	1mg	¥4945.45	请登录
PL09464-5mg	5mg	询价	询价
PL09464-10mg	10mg	询价	询价

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中文名称	PF-03654764
中文别名	3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutane-1-carboxamide
英文名称	PF-03654764
英文别名	H3 receptor antagonist 1;FPI2G03BJ1;Cyclobutanecarboxamide, 3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]-N-(2-methylpropyl)-, trans-;BDBM50401002;DB12360;Q27278116;trans-3-Fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (ACI);PF 03654764;PF-03654764
Cas No.	935840-35-0
分子式	C₂₀H₂₈F₂N₂O
分子量	350.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

PF-03654764 是一种具有口服活性的，选择性组胺 H₃ 受体拮抗剂，对人 H₃ 和大鼠 H₃ 的 K_i 值分别为 1.2 nM 和 7.9 nM。PF-03654764 和 Fexofenadine (HY-B0801A) 组合具有用于过敏性鼻炎研究的潜力。

生物活性

PF-03654764 is an orally active, selective histamine H 3 receptor antagonist with K i values of 1.2 nM and 7.9 nM for human H 3 and rat H 3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research.

性状

Solid

IC50 & Target[1][2]

human H3 receptor 1.2 nM (Ki) rat H3 receptor

体外研究(In Vitro)

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Travis T Wager, 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
[2]. Michelle L North, et al. Add-on histamine receptor-3 antagonist for allergic rhinitis: a double blind randomized crossover trial using the environmental exposure unit. Allergy Asthma Clin Immunol. 2014 Jul 3;10(1):33.

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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