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ARN272

Chemical Structure : ARN272

CAS No.: 488793-85-7

ARN272 (ARN-272)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 432.47
Formula C27H20N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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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