882366-16-7
中文名稱(chēng)
SBI-115; SBI 115; SBI115
英文名稱(chēng)
m-tolyl 5-chloro-2-(ethylsulfonyl)pyrimidine-4-carboxylate
CAS
882366-16-7
分子式
C14H13ClN2O4S
分子量
340.78
MOL 文件
882366-16-7.mol
更新日期
2025/01/15 10:03:29
882366-16-7 結(jié)構(gòu)式
基本信息
中文別名
SB-115游離化合物SBI-115
5-氯-2-(乙基磺?；?嘧啶-4-羧酸間甲苯酚酯
英文別名
SBI115SBI 115
SBI-115
SBI-115
SBI 115
SBI115
m-tolyl 5-chloro-2-(ethylsulfonyl)pyrimidine-4-carboxylate
3-Methylphenyl 5-chloro-2-(ethylsulfonyl)-4-pyrimidinecarboxylate
4-Pyrimidinecarboxylic acid, 5-chloro-2-(ethylsulfonyl)-, 3-methylphenyl ester
物理化學(xué)性質(zhì)
沸點(diǎn)529.7±60.0 °C(Predicted)
密度1.386±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,2-8°C
溶解度DMSO:109.0(Max Conc. mg/mL);319.86(Max Conc. mM)
酸度系數(shù)(pKa)-7.73±0.49(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
SBI-115 是一種新型的 TGR5 (GPCR19) 拮抗劑。SBI-115 在囊性膽管細(xì)胞中可抑制細(xì)胞增殖，降低膽管細(xì)胞球狀細(xì)胞的生長(zhǎng)速率和cAMP的水平。靶點(diǎn)
| Target | Value |
|
TGR5
() |
體外研究
SBI-115 (100-200 μM, 24 hours) inhibits proliferation triggered by pre-treatment of cystic cholangiocytes with Taurolithocholic acid (TLCA) in shRNA-transfected ADPKD cholangiocytes.
Cell Proliferation Assay
| Cell Line: | shRNA-transfected ADPKD cholangiocytes |
| Concentration: | 100, 200 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited proliferation (by 32-48%) triggered by pre-treatment of cystic cholangiocytes with TLCA. |