Sinbaglustat
(Synonyms: ACT-519276; OGT2378) 目录号 : GC68391Sinbaglustat (OGT2378) 是葡萄糖神经酰胺合成酶 (GCS) 和非溶酶体葡萄糖神经酰胺酶 (GBA2) 的双重抑制剂。Sinbaglustat 是一种可透过血脑屏障的的口服N-烷基亚氨基糖。Sinbaglustat 可用于与溶酶体功能障碍相关的中枢神经退行性疾病的研究。
Cas No.:441061-33-2
Sample solution is provided at 25 µL, 10mM.
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Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions[1][2].
Sinbaglustat (OGT2378; 20 μM) reduces the synthesis of glucosylceramide and ganglioside by 93% and >95% in MEB4 melanoma cells compared with untreated MEB4 cells, respectively, without either cytotoxic or antiproliferative effects[1].
GBA2 is an enzyme involved in the catabolism of glycosphingolipids (GSLs). Sinbaglustat is 50-fold more potent in inhibiting GBA2 than GCS[2].
Sinbaglustat (OGT2378; administered p.o., in the powdered chow, at a dose of 2500 mg/kg/day, corresponding to 35-40 mg of Sinbaglustat per mouse per day) is highly effective in impeding melanoma tumor growth in vivo. The effectiveness of p.o. Sinbaglustat in this murine model suggests that inhibition of glycosphingolipid synthesis is a promising approach to inhibit tumor progression[1].
| Animal Model: | Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor[1] |
| Dosage: | 35-40 mg per mouse per day |
| Administration: | Administered p.o., in the powdered chow, at a dose of 2500 mg/kg/day |
| Result: | Inhibited MEB4 melanoma tumor growth in a syngeneic, orthotopic murine model. |
[1]. Michael Weiss,et al. Inhibition of melanoma tumor growth by a novel inhibitor of glucosylceramide synthase. Cancer Res.2003 Jul 1;63(13):3654-8.
[2]. Martine Gehin,et al. Assessment of Target Engagement in a First-in-Human Trial with Sinbaglustat, an Iminosugar to Treat Lysosomal Storage Disorders. Clin Transl Sci.2021 Mar;14(2):558-567.
| Cas No. | 441061-33-2 | SDF | Download SDF |
| 别名 | ACT-519276; OGT2378 | ||
| 分子式 | C11H23NO4 | 分子量 | 233.3 |
| 溶解度 | DMSO : 83.33 mg/mL (357.18 mM; Need ultrasonic) | 储存条件 | Store at -20°C, away from moisture and 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2863 mL | 21.4316 mL | 42.8633 mL |
| 5 mM | 0.8573 mL | 4.2863 mL | 8.5727 mL |
| 10 mM | 0.4286 mL | 2.1432 mL | 4.2863 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet