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| | AKU-005 Basic information |
| Product Name: | AKU-005 | | Synonyms: | AKU-005;Methanone, [4-(diphenylmethyl)-1-piperazinyl]-1H-1,2,4-triazol-1-yl- | | CAS: | 1515855-85-2 | | MF: | C20H21N5O | | MW: | 347.41 | | EINECS: | | | Product Categories: | | | Mol File: | 1515855-85-2.mol |  |
| | AKU-005 Chemical Properties |
| Boiling point | 503.627±60.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.243±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 5.449±0.10(predicted) | | form | Solid | | color | White to off-white |
| | AKU-005 Usage And Synthesis |
| Uses | AKU-005 is a FAAH and MAGL dual inhibitor with IC50 values of 63, 389 nM for rat and human FAAH, respectively. AKU-005 has the potential for the research of trigeminal hyperalgesia[1][2]. | | in vivo | AKU-005 (0.5 mg/kg; i.p.) shows anti-hyperalgesic and anti-inflammatory effects in rats[1]. | Animal Model: | 150-175 g, Male Sprague Dawley rats (NTG 10 mg/kg; i.p.)[1] | | Dosage: | 0.5 mg/kg | | Administration: | I.p.; 3 h after NTG (nitroglycerin) | | Result: | Significantly prevented the NTG-induced increase in face-rubbing behavior, decreased the CGRP mRNA levels in the meninges, medulla, CSC, and TG ipsilateral, prevented an NTG-induced increase in IL-6 and TNF-alpha mRNA levels in all areas, except for TNF-alpha in the medulla. |
| | References | [1] Greco R, et al. Effects of the Dual FAAH/MAGL Inhibitor AKU-005 on Trigeminal Hyperalgesia in Male Rats. Cells. 2024 May 13;13(10):830. DOI:10.3390/cells13100830
[2] Aaltonen N, et al. Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem Biol. 2013 Mar 21;20(3):379-90. DOI:10.1016/j.chembiol.2013.01.012 |
| | AKU-005 Preparation Products And Raw materials |
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