Glucosylceramide synthase-IN-1|2601393-20-6|(Glucosylceramide synthase-IN-1)-陌孚医药/Medlife

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Glucosylceramide synthase-IN-1 (Synonyms: Glucosylceramide synthase-IN-1)

目录号: PL04020 纯度: ≥99%

CAS No. :2601393-20-6

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中文名称	Glucosylceramide synthase-IN-1
英文名称	Glucosylceramide synthase-IN-1
英文别名	1H-Pyrrolo[3,4-c]pyridin-1-one, 4-[4-fluoro-2-(2,2,2-trifluoroethoxy)phenyl]-2,3-dihydro-2-[4-(1-hydroxy-1-methylethyl)phenyl]-
Cas No.	2601393-20-6
分子式	C₂₄H₂₀F₄N₂O₃
分子量	460.42
包装储存	4°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)

产品详情	Glucosylceramide synthase-IN-1 (T-036) 是一种有效的、可穿过血脑屏障的和具有口服活性的 glucosylceramide synthase (GCS) 抑制剂，对人 GCS 和小鼠 GCS 的 IC₅₀ 分别为 31 nM 和 51 nM。Glucosylceramide synthase-IN-1 可用于戈谢病研究。
生物活性	Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC 50 s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gauchers disease research.
性状	Solid
IC50 & Target[1][2]	IC50: 31 nM (human GCS) and 51 nM (mouse GCS)
体外研究(In Vitro)	Glucosylceramide synthase-IN-1 (T-036) potently reduces the GCS product, catalyze glucosylceramide (GlcCer), in the fibroblasts with Gaucher’s disease (EC50 of 7.6 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Glucosylceramide synthase-IN-1 (T-036) has good oral exposure (BA = 67%) and moderate brain penetration ( Kpuu,brain = 0.11). Administration of a single dose of Glucosylceramide synthase-IN-1 (T-036) reduces GlcCer in the plasma and cerebral cortex of wild-type mice, and administration of Glucosylceramide synthase-IN-1 (T-036) for 2 months significantly reduces glucosylsphingosine (GlcSph) in the cerebral cortex of the Gaucher’s disease mouse model. 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	4°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]. Yuta Tanaka, et al. Discovery of Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore. J Med Chem. 2022 Mar 10;65(5):4270-4290

溶解度数据	In Vitro: DMSO : 100 mg/mL (217.19 mM; Need ultrasonic)配制储备液

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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。

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