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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-FAAH-ARN272
ARN272

Chemical Structure : ARN272

CAS No.: 488793-85-7

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ARN272 (ARN-272)

货号: PC-38511Not For Human Use, Lab Use Only.

ARN272 (ARN-272) is a specific, competitive FAAH-like anandamide transporter (FLAT) inhibitor, antagonizes [3H]-anandamide binding to purified FLAT (IC50=1.8 uM) and inhibits [3H]-anandamide accumulation in FLAT-expressing HEK293 cells with IC50 of 3 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ARN272 (ARN-272) is a specific, competitive FAAH-like anandamide transporter (FLAT) inhibitor, antagonizes [3H]-anandamide binding to purified FLAT (IC50=1.8 uM) and inhibits [3H]-anandamide accumulation in FLAT-expressing HEK293 cells with IC50 of 3 uM.
ARN272 (1 mg/kg intraperitoneal, i.p.) in mice increased plasma levels of anandamide without changing the levels of 2-AG, OEA or PE.
ARN272 produces CB1-dependent antinociception, attenuates nociceptive and inflammatory pain in mice.
ARN272 tonically activates CB1 receptors and as such produces a type of indirect agonism to regulate toxin-induced nausea and vomiting.
FAAH-like anandamide transporter (FLAT) is a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1).
FLAT was proposed to function as an intracellular AEA carrier and mediate its delivery to FAAH for hydrolysis. Pharmacological inhibition of FLAT potentiated AEA signaling and produced antinociceptive effects.

物理化学性质&存储条件

分子量 432.47
分子式 C27H20N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-[[4-(4-Hydroxyphenyl)-1-phthalazinyl]amino]-N-phenylbenzamide

参考文献

1. Fu J, et al. Nat Neurosci. 2011 Nov 20;15(1):64-9.

2. O'Brien LD, et al. Br J Pharmacol. 2013 Nov;170(5):1130-6.

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