| KT182ABHD6 (a/b-Hydrolase Domain Containing 6) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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| Cas No. | 1402612-62-7 | SDF | Download SDF |
| Chemical Name | [4-[3"-(hydroxymethyl)[1,1"-biphenyl]-4-yl]-1H-1,2,3-triazol-1-yl](2-phenyl-1-piperidinyl)-methanone | ||
| Canonical SMILES | O=C(N1N=NC(C2=CC=C(C3=CC=CC(CO)=C3)C=C2)=C1)N4C(C5=CC=CC=C5)CCCC4 | ||
| Formula | C27H26N4O2 | M.Wt | 438.5 |
| Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: < 5="">
KT182 is an ABHD6 inhibitor.
α/β-Hydrolase domain containing 6 (ABHD6), a transmembrane serine hydrolase, hydrolyzes the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) to regulate certain forms of cannabinoid receptor-dependent signaling in the nervous system.
In vitro: The in-vitro potencies were tested for KT182 and the results found that KT182 could potently inhibit ABHD6 as measured by gelbased competitive ABPP and 2-AG hydrolysis assays. Moreover, the in-situ potencies were measured by treating Neuro2A cells with varying concentrations of KT182 for 4 h, and it was found that KT182 could inhibit ABHD6 with IC50 values in the subnanomolar range [1].
In vivo: In animal study, mice were treated intraperitoneally with KT182 at various doses (0.1-1 mg/kg) for 4 h, and the results found that KT182 could produce near-complete blockade of ABHD6 in the liver at the highest dose tested. Moreover, KT182 at lower doses maintained around 80% inhibition of ABHD6 in the liver and KT182 at higher doses showed impressive selectivity in the mouse liver, exhibiting little cross-reactivity against the numerous carboxylesterase enzymes. In addition, KT182 could also completely inactivate ABHD6 in the mouse brain at 1 mg/kg [1].
Clinical trial: Up to now, KT182 is still in the preclinical development stage.
Reference:[1] Hsu KL, Tsuboi K, Chang JW, Whitby LR, Speers AE, Pugh H, Cravatt BF. Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6). J Med Chem. 2013 Nov 14;56(21):8270-9.
