A939572
(Synonyms: 4-(2-氯苯氧基)-N-[3-[(甲胺基)羰基]苯基]-1-哌啶羧胺) 目录号 : GC15921
A stearoyl-CoA desaturase 1 inhibitor
Cas No.:1032229-33-6
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
| Animal experiment [1]: | |
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Animal models |
ob/ob mice |
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Dosage form |
10 mg/kg; b.i.d. |
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Applications |
In ob/ob mice, A939572 lowered the desaturation index (18:0/18:1n9). Moreover, A939572 reduced triglyceride desaturation index in a dose-dependent manner. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302. | |
A939572 is a potent and orally bioavailable inhibitor of stearoyl-CoA desaturase1 (SCD1) with IC50 value of 37nM [1].
SCD is a microsomal enzyme that catalyzes the biosynthesis of monounsaturated fatty acids. One member of SCD family, SCD1, is regulated by dietary and hormonal factors and is proved to play an important role in lipid metabolism and body weight control. Thus, SCD1 is a target for the treatment of obesity and diabetes. A939572 is a synthetic inhibitor of SCD1 with improved inhibitory activity and lipophilicity than its parent compound. It shows inhibition of mouse SCD1 and human SCD1 with IC50 values of <4nM and 37nM, respectively. In addition, A939572 has no inhibitory activity to the co-enzymes of SCD1, cytochrome b5 and cytochrome b5 reductase. It suggests that A939572 interacts with SCD1 directly and specifically. Furthermore, A939572 shows high oral bioavailability in mice [1].
References:
[1] Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302.
| Cas No. | 1032229-33-6 | SDF | |
| 别名 | 4-(2-氯苯氧基)-N-[3-[(甲胺基)羰基]苯基]-1-哌啶羧胺 | ||
| 化学名 | 4-(2-chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide | ||
| Canonical SMILES | CNC(C1=CC(NC(N2CCC(OC3=CC=CC=C3Cl)CC2)=O)=CC=C1)=O | ||
| 分子式 | C20H22ClN3O3 | 分子量 | 387.86 |
| 溶解度 | ≥ 17.15mg/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。 |
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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 | 2.5782 mL | 12.8912 mL | 25.7825 mL |
| 5 mM | 0.5156 mL | 2.5782 mL | 5.1565 mL |
| 10 mM | 0.2578 mL | 1.2891 mL | 2.5782 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。