JZP-430
目录号 : GC34640
An ABHD6 inhibitor
Cas No.:1672691-74-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
JZP 430 is an inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 0.044 for the human enzyme).1 It is selective for ABHD6 over fatty acid amid hydrolase (FAAH) and monoacylglycerol lipase (MAGL) when used at a concentration of 2.5 ?M, ABHD12 at 1 ?M, as well as lysosomal acid lipase (LAL) and cannabinoid 1 (CB1) and CB2 receptors at 10 ?M.
1.Patel, J.Z., Nevalainen, T.J., Savinainen, J.R., et al.Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitorsChemMedChem10(2)253-265(2015)
| Cas No. | 1672691-74-5 | SDF | |
| Canonical SMILES | O=C(OC1=NSN=C1N2CCOCC2)N(C3CCCCCCC3)C | ||
| 分子式 | C16H26N4O3S | 分子量 | 354.47 |
| 溶解度 | DMSO : 100 mg/mL (282.11 mM; Need ultrasonic) | 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。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8211 mL | 14.1056 mL | 28.2111 mL |
| 5 mM | 0.5642 mL | 2.8211 mL | 5.6422 mL |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8211 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。
Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors
ChemMedChem 2015 Feb;10(2):253-65.PMID:25504894DOI:PMC4471478
At present, inhibitors of α/β-hydrolase domain 6 (ABHD6) are viewed as a promising approach to treat inflammation and metabolic disorders. This article describes the development of 1,2,5-thiadiazole carbamates as ABHD6 inhibitors. Altogether, 34 compounds were synthesized, and their inhibitory activity was tested using lysates of HEK293 cells transiently expressing human ABHD6 (hABHD6). Among the compound series, 4-morpholino-1,2,5-thiadiazol-3-yl cyclooctyl(methyl)carbamate (JZP-430) potently and irreversibly inhibited hABHD6 (IC50 =44 nM) and showed ∼230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL), the main off-targets of related compounds. Additionally, activity-based protein profiling indicated that JZP-430 displays good selectivity among the serine hydrolases of the mouse brain membrane proteome. JZP-430 has been identified as a highly selective, irreversible inhibitor of hABHD6, which may provide a novel approach in the treatment of obesity and type II diabetes.