| 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%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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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. | ||
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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.
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1、 缓冲溶液对反应物的测定没有干扰
2、缓冲组分的浓度为1:1
3、有足够的缓冲容量
4、缓冲溶液的PH应在所需范围内
5、组成缓冲溶液的弱碱PKB和弱酸PKA应接近或等于所需的POH值或PH值（PH+POH=14）
配制
只要知道缓冲对的PH值，和要配制的缓冲液的pH值（及要求的缓冲液总浓度），就能按公式计算[盐]和[酸]的量。这个算法涉及对数换算，较麻烦，前人为减少后人的计算麻烦，已为我们总结出pH值与缓冲液对离子用量的关系并列出了表格。只要我们知道要配制的缓冲液的pH，经查表便可计算出所用缓冲剂的比例和用量。例如配制500nmpH5.8浓度为0.1M磷酸缓冲液。
经查表知pH5.8浓度为0.2M Na2HPO48.0毫升，而0.2M Na2HPO492.0毫升。依此可推论出配制100ml0.1M的磷酸缓冲液需要0.1M Na2HPO48.0毫升，而0.1M Na2HPO4需要92.0毫升。
计算好后，按计算结果准确称好固态化学成分，放于烧杯中，加少量蒸馏水溶解，转移入50ml容量瓶，加蒸馏水至刻度，摇匀，就能得到所需的缓冲液。
各种缓冲溶液的配制，均按表格按比例混合，某些试剂，必须标定配成准确浓度才能进行，如醋酸、氢氧化钠等。另外，所有缓冲溶剂的配制计量都能从以上的算式准确获得。
TBST中含有Tris-Hcl，NaCl，Tween20这三种物质，是做WESTERNBLOT中常用的一种缓冲液。
TBST缓冲液的配制
1000ml×TBST的配置
先称量NaCl40g，倒入烧杯中，加DDW蒸馏水400ml,再称量NaCl47.6g，倒入刚才的那个烧杯中（PS：由于NaCl的量太多，一次称量不方便，所以分两次称量，且易于溶解）。往烧杯中加入Tris—HCl缓冲液100ml，最后加（吐温20）5ml,转入1000ml容量瓶中，在定容，转移即可。
TBST缓冲液的应用：
1.主要用于免疫组化和原位杂交，酶联免疫等实验中，清洗免疫印。
2.迹膜；
注意事项：
1.TBST缓冲液，PH7.2-7.5；
2.颜色为无色透明液体；
3.为了您的安全和健康，请穿实验服并戴防护手套操作；
