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Sinbaglustat

(Synonyms: ACT-519276; OGT2378)

目录号: PL11706 纯度: ≥98%

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。

CAS No. :441061-33-2

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中文名称	Sinbaglustat
中文别名	SINBAGLUSTAT
英文名称	Sinbaglustat
英文别名	3,4,5-PIPERIDINETRIOL, 2-(HYDROXYMETHYL)-1-PENTYL-, (2S,3R,4R,5S)-;OGT2378;ACT-519276;Sinbaglustat
Cas No.	441061-33-2
分子式	C₁₁H₂₃NO₄
分子量	233.31
包装储存	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述	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。

产品详情	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.
性状	Solid
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献	[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.

溶解度数据	In Vitro: DMSO : 83.33 mg/mL (357.18 mM; Need ultrasonic)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Sinbaglustat

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