154563-54-9
中文名稱(chēng)
N-[3,5-Bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)-5-pyrimidinecarboxamide
英文名稱(chēng)
N-[3,5-Bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)-5-pyrimidinecarboxamide
CAS
154563-54-9
分子式
C14H5ClF9N3O
分子量
437.65
MOL 文件
154563-54-9.mol
更新日期
2023/03/20 15:41:27
154563-54-9 結(jié)構(gòu)式
基本信息
中文別名
化合物 T24816化合物SP-100030
英文別名
SP 100030N-[3,5-Bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)-5-pyrimidinecarboxamide
5-Pyrimidinecarboxamide, N-[3,5-bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)-
物理化學(xué)性質(zhì)
熔點(diǎn)166-167 °C
沸點(diǎn)340.6±42.0 °C(Predicted)
密度1.637±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)8.97±0.70(Predicted)
形態(tài)Solid
顏色Off-white to light yellow
常見(jiàn)問(wèn)題列表
生物活性
SP-100030 是一種有效的 NF-κB 和激活蛋白-1 (AP-1) 雙抑制劑 (IC50 分別為 50 和 50 nM)。SP-10003 抑制 Jurkat和其他T細(xì)胞系產(chǎn)生的 IL-2、IL-8 和 TNF-α 的產(chǎn)生。SP-100030 降低小鼠膠原性關(guān)節(jié)炎 (CIA)。體外研究
SP-100030 blocks the production of IL-2 and IL-8 in Jurkat T-cells at the same concentrations as seen in the luciferase assay (IC
50
≈30 nM).
ELISA and RT-PCR confirmed that IL-2, IL-8, and TNF-alpha production by activated Jurkat and other T cell lines were inhibited by SP100030.
體內(nèi)研究
SP100030 (10 mg/kg/day; i.p.; day 21 to day 34) significantly decreased arthritis severity.
| Animal Model: | Six- to 8-wk-old male DBA/1J mice (immunized with type II collagen) |
| Dosage: | 10 mg/kg |
| Administration: | I.p.; daily, starting at day 21 to the end of the study on day 34 |
| Result: | Significantly decreased arthritis scores compared with controls; Histologic evaluation of the paws from mice treated from day 20 to 34 showed a trend toward decreased inflammation. |