Sinbaglustat ACT-519276; OGT2378|cas:441061-33-2|西域试剂

Sinbaglustat ACT-519276; OGT2378

产品编号：Bellancom-129411| CAS NO：441061-33-2| 分子式：C₁₁H₂₃NO₄| 分子量：233.30

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-129411		￥5800.00	杭州北京（现货）
Bellancom-129411		￥9800.00	杭州北京（现货）

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Sinbaglustat ACT-519276; OGT2378

产品介绍

Sinbaglustat (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。

生物活性

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.

体外研究

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.
GBA2 is an enzyme involved in the catabolism of glycosphingolipids (GSLs). Sinbaglustat is 50-fold more potent in inhibiting GBA2 than GCS.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (357.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6.25 mg/mL (26.79 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (26.79 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液