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Chemical Structure : ARN272
CAS No.: 488793-85-7
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $268 | In stock | |
| 50 mg | $458 | In stock | |
| 100 mg | $788 | In stock | |
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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.
| M.Wt | 432.47 | |
| Formula | C27H20N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-[[4-(4-Hydroxyphenyl)-1-phthalazinyl]amino]-N-phenylbenzamide |
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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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