PF-04457845|1020315-31-4|(PF-04457845)-陌孚医药/Medlife

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PF-04457845 (Synonyms: PF-04457845)

目录号: PL04009 纯度: ≥99%

CAS No. :1020315-31-4

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中文名称	PF-04457845
中文别名	N-哒嗪-3-基-4-(3-{[5-(三氟甲基)吡啶-2-基]醚}苯亚甲基丙酮)哌啶-1-羧酰胺
英文名称	PF-04457845
英文别名	2H-Cyclopenta[b]furan-2-one, 5-(benzoyloxy)-4-[(1E)-3,3-difluoro-4-phenoxy-1-butenyl]hexahydro-, (3aR,4R,5R,6aS)-;2H-Cyclopenta[b]furan-2-one, 5-(benzoyloxy)-4-[(1E)-3,3-difluoro-4-phenoxy-1-butenyl]hexahydro...;N-pyridazin-3-yl-4-[[3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl]methylidene]piperidine-1-carboxamide;CHEBI:1163958;CHEMBL1651534;CS-0868;HY-14376;N-pyridazin-3-yl-4-(3-{[5-(trifluoromethyl)pyridin-2-yl]oxy}benzylidene)piperidine-1-carboxamide;SureCN1010408;UNII-H4C81M8YYW;N-(3-pyridazinyl)-4-(3-[5-trifluoromethyl-2-pyridinyloxy]benzylidene)piperidine-1-carboxamide;N-3-Pyridazinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methylene]-1-piperidinecarboxamide;PF-4457845;1-Piperidinecarboxamide, n-3-pyridazinyl-4-[[3-[[5-(trifluoromethyl)-2- pyridinyl]oxy]phenyl]methylene]-;PF 04457845;H4C81M8YYW;PF04457845;C23H20F3N5O2;N-Pyridazin-3-yl-4-((3-(5-(trifluoromethyl)pyridin-2-yl)oxyphenyl)methylidene)piperidine-1-carboxamide;1-Piperidinecarboxamide, N-3-pyridazinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methylene]-;1-Piperidinecarboxamide, N-3-pyridazinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]me;PF-04457845;N-Pyridazin-3-yl-4-(3-{[5-(trifluoroMethyl)pyridin-2-yl]oxy}benzylidene)piperidine-1-carboxaMide
Cas No.	1020315-31-4
分子式	C₂₃H₂₀F₃N₅O₂
分子量	455.43
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

PF-04457845 是一种高效选择性的 FAAH 抑制剂，作用于 hFAAH 和 rFAAH，IC₅₀ 分别为 7.2±0.63 nM 和 7.4±0.62 nM。

生物活性

PF-04457845 is a highly efficacious and selective FAAH inhibitor with IC 50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 7.2±0.63 nM (hFAAH), 7.4±0.62 nM (rFAAH)

体外研究(In Vitro)

PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (kinact/Ki and IC50 values of 40300 Ms and 7.2 nM, respectively, for human FAAH). PF-04457845 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. PF-04457845 completely inhibits FAAH in human and mouse membrane proteomes at both 10 and 100 μM with no off targets. PF-04457845 is completely selective for FAAH, and none of the other FP-reactive serine hydrolases in the tested tissues are inhibited by PF-04457845 even at 100 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Oral administration of PF-04457845 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Oral administration of PF-04457845 causes a significant inhibition of mechanical allodynia measured after 4 h with a minimum effective dose (MED) of 0.1 mg/kg. Furthermore, at 0.1 mg/kg (p.o.), PF-04457845 inhibits the pain response to a comparable degree as the nonsteroidal anti-inflammatory drug naproxen at 10 mg/kg. FAAH is confirmed to be completely inhibited in mice treated with PF-04457845 at 1 and 10 mg/kg p.o. by competitive activity-based protein profiling (ABPP) study. 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]. Johnson DS, et al. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med Chem Lett. 2011 Feb 10;2(2):91-96.
[2]. Ahn K, et al. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J Pharmacol Exp Ther. 2011 Jul;338(1):114-24.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (219.57 mM)配制储备液

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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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