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。

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 Gaucher's disease research [1].

Glucosylceramide synthase-IN-2 (compound T-690) has no SERT inhibitory activity (IC 50 >10 μM). Glucosylceramide synthase-IN-2 does not affect GCase activity (EC 50 >300 μM) [1]. Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, Ca V 1.2, and Na V 1.5 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 max of 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].

2597958-02-4

C22H20F3N3O4

447.41

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years