Glucosylceramide synthase-IN-2

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Glucosylceramide synthase-IN-2

CAS No. : 2597958-02-4

MCE 国际站：Glucosylceramide synthase-IN-2

产品活性：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。

研究领域：Neuronal Signaling

作用靶点：Glucosylceramide Synthase (GCS)

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, Ca_V1.2, and Na_V1.5 channels.

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).

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