PF-3845 - Moligand™, 10mM in DMSO , Inhibitor of Fatty acid amide hydrolase, CAS No.1196109-52-0, Inhibitor of Fatty acid amide hydrolase

CAS: 1196109-52-0 Cat. No.: P408694 分子式: C₂₄H₂₃F₃N₄O₂ EC番号: 802-455-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

PF-3845 PF-3845 is a potent, selective and irreversible FAAH inhibitor with K i of 230 nM, showing negligible activity against FAAH2.
In vitro

PF-3845 selectively inhibits FAAH by carbamylating FAAH\'s serine nucleophile.

In vivo

PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater,degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.). PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn\'t modify paw withdrawal thresholds in the saline-injected paw.
Cell Data

cell lines：NCI-H929, U266, RPMI-8226 and OPM2 MM cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

同義語

4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

PF-3845 is a potent, selective and irreversible FAAH inhibitor with K_i of 230 nM, showing negligible activity against FAAH2.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of Fatty acid amide hydrolase

名前と識別子

• 異性体SMILES: C1CN(CCC1CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=CN=CC=C4
• WGKドイツ: 3
• Reaxy-Rn: 20599234
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20599234&ln=

関連ターゲット（人間）

FAAH Tchem Fatty-acid amide hydrolase 1 (2 Activities)

Discover Target: FAAH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)