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.
体内研究
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 ED50s 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%).
分子式
C20H22F6N4O4S
分子量
528.47
CAS号
2414349-93-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20˚C, stored under nitrogen, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶解性数据
In Vitro:
DMSO : 115 mg/mL (217.61 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.8923 mL
9.4613 mL
18.9226 mL
5 mM
0.3785 mL
1.8923 mL
3.7845 mL
10 mM
0.1892 mL
0.9461 mL
1.8923 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: