FAAH inhibitor 1
(Synonyms: Benzothiazole analog 3) 目录号 : GC36023FAAH inhibitor 1是脂肪酸酰胺水解酶(FAAH)抑制剂,IC50为18 nM。
Cas No.:326866-17-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
FAAH inhibitor 1 is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.IC50 Value: 18±8 nM [1]Target: FAAHTime-dependent preincubation study of FAAH inhibitor 1 was consistent with it being a reversible inhibitor. Activity-based protein-profiling (ABPP) evaluation of FAAH inhibitors 1 in rat tissues revealed that it had exceptional selectivity and no off-target activity with respect to other serine hydrolases. Molecular shape overlay of FAAH inhibitor 1 with a known FAAH inhibitor indicated that these compounds might act as transitionstate analogues, forming putative hydrogen bonds with catalytic residues and mimicking the charge distribution of the tetrahedral transition state. FAAH inhibitors 1 was exclusively specific against FAAH in rat brain and had no missing protein bands in all the other tissues that were tested [1].
[1]. Wang, Xueqing; Sarris, Katerina; Kage, Karen; et al. Synthesis and Evaluation of Benzothiazole-Based Analogues as Novel, Potent, and Selective Fatty Acid Amide Hydrolase Inhibitors. Journal of Medicinal Chemistry (2009), 52(1), 170-180. [2]. Meyers, Marvin J.; Long, Scott A.; Pelc, Matthew J.; et al. Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: Identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds. Bioorganic & Medicinal Chemistry Letters (2011), 21(21), 6538-6544.
Cas No. | 326866-17-5 | SDF | |
别名 | Benzothiazole analog 3 | ||
Canonical SMILES | CC1=CC=C(N=C(C2=CC=C(NC(C3CCN(S(=O)(C4=CC=CS4)=O)CC3)=O)C=C2)S5)C5=C1 | ||
分子式 | C24H23N3O3S3 | 分子量 | 497.65 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C,protect from light |
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。 |
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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 | 2.0094 mL | 10.0472 mL | 20.0944 mL |
5 mM | 0.4019 mL | 2.0094 mL | 4.0189 mL |
10 mM | 0.2009 mL | 1.0047 mL | 2.0094 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。