Genz-123346 free base
(Synonyms: N-[(1R,2R)-1-(2,3-二氢苯并[B][1,4]二恶英-6-基)-1-羟基-3-(吡咯烷-1-基)丙-2-基]壬酰胺) 目录号 : GC36133
A glucosylceramide synthase inhibitor
Cas No.:491833-30-8
Sample solution is provided at 25 µL, 10mM.
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Genz-123346 is a glucosylceramide synthase inhibitor (IC50 = 14 nM).1 It reduces hepatic levels of glucosylceramide and triglycerides as well as blood levels of alanine aminotransferase (ALT), hemoglobin A1c, and non-fasting glucose in ob/ob mice when administered at a dose of 120 mg/kg per day.2 Genz-123346 (125 mg/kg per day) also decreases hepatic fat mass and reduces the size and number of hepatic lipid droplets in diet-induced obese mice.
1.Zhao, H., Przybylska, M., Wu, I.-H., et al.Inhibiting glycosphingolipid synthesis improves glycemic control and insulin sensitivity in animal models of type 2 diabetesDiabetes56(5)1210-1218(2007) 2.Zhao, H., Przybylska, M., Wu, I.-H., et al.Inhibiting glycosphingolipid synthesis ameliorates hepatic steatosis in obese miceHepatology50(1)85-93(2009)
Animal experiment: | Rats: Genz-123346 is dissolved in water. Zucker diabetic fatty rats treated with Genz-123346 (75 mg/kg) for 6 weeks are fasted overnight. The following morning, the fasted rats are anesthetized and injected with 5 units human insulin into the hepatic portal vein. Quadriceps muscle and liver are harvested 2 min after injection and immediately frozen in liquid nitrogen. Insulin receptor is immunoprecipitated. The immunoprecipitates are analyzed by immunoblotting[1]. Mice: C57BL/6 mice are fed on a high-fat (45% of kcal) diet for 8 weeks, obese mice with comparable body weight gain, glucose, and insulin levels are assigned to either the treated or control groups. The mice are then gavaged daily with Genz-123346 or water for 10 weeks[1]. |
References: [1]. Zhao H, et al. Inhibiting glycosphingolipid synthesis improves glycemic control and insulin sensitivity in animal models of type 2 diabetes. Diabetes. 2007 May;56(5):1210-8. | |
| Cas No. | 491833-30-8 | SDF | |
| 别名 | N-[(1R,2R)-1-(2,3-二氢苯并[B][1,4]二恶英-6-基)-1-羟基-3-(吡咯烷-1-基)丙-2-基]壬酰胺 | ||
| Canonical SMILES | CCCCCCCCC(N[C@H](CN1CCCC1)[C@@H](C2=CC=C(OCCO3)C3=C2)O)=O | ||
| 分子式 | C24H38N2O4 | 分子量 | 418.57 |
| 溶解度 | DMSO: ≥ 100 mg/mL (238.91 mM) | 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 | 2.3891 mL | 11.9454 mL | 23.8909 mL |
| 5 mM | 0.4778 mL | 2.3891 mL | 4.7782 mL |
| 10 mM | 0.2389 mL | 1.1945 mL | 2.3891 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet