Glucosylceramide synthase-IN-2

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CAS NO:	2597958-02-4
包装:	10mg
市场价:	7200元

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。

Cas No.	2597958-02-4
分子式	C₂₂H₂₀F₃N₃O₄
分子量	447.41
储存条件	4°C, away from moisture and light
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally activeglucosylceramide synthase (GCS)inhibitor withIC₅₀s 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 Gaucher's disease research^[1]. 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)^[1]. Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, Ca_V1.2, and Na_V1.5 channels^[1]. 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^[1]. Glucosylceramide synthase-IN-2 (po; 5 mg/kg) has a C_maxof 416 ng/mL. Glucosylceramide synthase-IN-2 shows good oral exposure (BA = 31%)^[1]. Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 μM at 30 mg/kg dosing, 1 h)^[1].