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KT182
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KT182图片
CAS NO:1402612-62-7
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt438.5
Cas No.1402612-62-7
FormulaC27H26N4O2
Solubility≤10mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name[4-[3'-(hydroxymethyl)[1,1'-biphenyl]-4-yl]-1H-1,2,3-triazol-1-yl](2-phenyl-1-piperidinyl)-methanone
Canonical SMILESO=C(N1N=NC(C2=CC=C(C3=CC=CC(CO)=C3)C=C2)=C1)N4C(C5=CC=CC=C5)CCCC4
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

IC50:< 5 nM

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.