WWL123
目录号 : GC15209A selective inhibitor of ABHD6
Cas No.:1338575-41-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.43 μM
WWL123 is a brain-penetrant inhibitor of ABHD6.
The serine hydrolase a/b-hydrolase domain 6 (ABHD6) has been reported to hydrolyze the most abundant endocannabinoid (eCB) in the brain, 2-arachidonoylglycerol (2-AG), and controls its availability at cannabinoid receptors.
In vitro: WWL123 was identified as a brain-penetrant inhibitor of ABHD6 demonstrating over 10-fold selectivity for ABHD6 compared to a panel of about 35 other serine hydrolases [1].
In vivo: In previous study, mice were pretreated with either vehicle or WWL123, and then they were treated with 50 mg/kg PTZ. It was found that pretreatment with WWL123 could block seizure-related mortality, reduce the severity of seizure behaviors, reduce the number of GTC seizures per mouse, and reduce the frequency of myoclonic (MC) seizures as well. In addition, to test whether behavioral seizures exhibited by R6/2 mice are controlled by chronic blockade of the eCB signaling system, the authors treated mice with a daily injection of vehicle, SR1, or WWL123. Results showed that WWL123 blocked the incidence of spontaneous behavioral seizures in R6/2 mice and there was no effect on duration of spontaneous seizures in response to chronic SR1 treatment vehicle [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Bachovchin, D. A.,Ji, T.,Simon, G.M., et al. Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening. Proceedings of the National Academy of Sciences of the United States of America 107(49), 20941-20946 (2010).
[2] Naydenov, A. V.,Horne, E.A.,Cheah, C.S., et al. ABHD6 blockade exerts antiepileptic activity in PTZ-induced seizures and in spontaneous seizures in R6/2 mice. Neuron 83(2), 361-371 (2014).
Cas No. | 1338575-41-9 | SDF | |
化学名 | N-([1,1'-biphenyl]-3-ylmethyl)-N-methyl-carbamic acid, 4'-(aminocarbonyl)[1,1'-biphenyl]-3-yl ester | ||
Canonical SMILES | O=C(N)C1=CC=C(C2=CC(OC(N(C)CC3=CC=CC(C4=CC=CC=C4)=C3)=O)=CC=C2)C=C1 | ||
分子式 | C28H24N2O3 | 分子量 | 436.5 |
溶解度 | ≤1mg/ml in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.291 mL | 11.4548 mL | 22.9095 mL |
5 mM | 0.4582 mL | 2.291 mL | 4.5819 mL |
10 mM | 0.2291 mL | 1.1455 mL | 2.291 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。