UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders.
性状
Solid
体内研究(In Vivo)
UGT8-IN-1 (compound 19) exhibits the T1/2 of 4.3 h, 1.13 h and 13.6 h by iv (1 mg/kg) administration in rat, mouse and dog, respectively. UGT8-IN-1 (compound 19) shows F% of 40%, 34% and 52% by oral (3 mg/kg) administration in rat, mouse and dog, respectively.
UGT8-IN-1 (compound 19, orally twice a day for three days) shows ≥90% inhibition of incorporation of C-Gal into GalCer and SFT, at all three doses tested, with the estimated ED 50 s of <3 mg/kg for inhibition of both SFT and GalCer. UGT8-IN-1 (compound 19) has very high plasma protein and tissue binding (>99%). 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, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
参考文献
[1]. Sukanthini Thurairatnam, et al. Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders. ACS Med Chem Lett. 2020 Jun 16;11(10):2010-2016.
溶解度数据
In Vitro: DMSO : 115 mg/mL (217.61 mM; Need ultrasonic)配制储备液
[1]. Sukanthini Thurairatnam, et al. Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders. ACS Med Chem Lett. 2020 Jun 16;11(10):2010-2016.