Glucosylceramide synthase-IN-2|2597958-02-4|-陌孚医药/Medlife

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Glucosylceramide synthase-IN-2

目录号: PL04021 纯度: ≥98%

CAS No. :2597958-02-4

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中文名称	Glucosylceramide synthase-IN-2
英文名称	Glucosylceramide synthase-IN-2
英文别名	Glucosylceramide synthase-IN-2
Cas No.	2597958-02-4
分子式	C₂₂H₂₀F₃N₃O₄
分子量	447.41
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-2 (compound T-690) 是一种有效的、可透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 15 nM 和 190 nM。Glucosylceramide synthase-IN-2 非竞争性抑制 C8 神经酰胺和 UDP 葡萄糖。Glucosylceramide synthase-IN-2 可用于戈谢病研究。
生物活性	Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC 50 s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gauchers disease research.
性状	Solid
体外研究(In Vitro)	Glucosylceramide synthase-IN-2 (compound T-690) has no SERT inhibitory activity (IC50>10 μM). Glucosylceramide synthase-IN-2 does not affect GCase activity (EC50>300 μM). Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, CaV1.2, and NaV1.5 channels. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Glucosylceramide synthase-IN-2 (compound T-690; po; 30, 100, 300 mg/kg) reduces GlcCer concentrations in the plasma and cerebral cortex in a dose-dependent manner in C57BL/6J mice. Glucosylceramide synthase-IN-2 (po; 5 mg/kg) has a C max of 416 ng/mL. Glucosylceramide synthase-IN-2 shows good oral exposure (BA = 31%). Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 μM at 30 mg/kg dosing, 1 h). 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 (223.51 mM; Need ultrasonic)配制储备液

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