2123480-72-6
中文名稱
UbcH5c-IN-6d
英文名稱
UbcH5c-IN-6d
CAS
2123480-72-6
分子式
C22H21BrO3
分子量
413.3
MOL 文件
2123480-72-6.mol
2123480-72-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 T13242 英文別名
UbcH5c-IN-1UbcH5c-IN-6d
UbcH5c IN 1,UbcH5cIN1,UbcH-5c-IN-1
Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3a,4,5,9b-tetrahydro-6,9-dimethyl-3-methylene-, (3aS,9bR)-
物理化學(xué)性質(zhì)
沸點(diǎn)559.8±50.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
常見問題列表
生物活性
UbcH5c-IN-1 (compound 6d) 是一種有效的、選擇性的小分子泛素結(jié)合酶 UbcH5c 抑制劑,其與 E2 UbcH5c-IN-1 活性位點(diǎn)Cys85共價(jià)結(jié)合的 Kd 值為 283 nM,是開發(fā)新型類風(fēng)濕性關(guān)節(jié)炎藥物的先導(dǎo)化合物。靶點(diǎn)
Kd: 283 nM (E2 UbcH5c).
體內(nèi)研究
UbcH5c-IN-1 (compound 6d) (5 and 20 mg/kg, p.o., daily, 10-20 days) treatment in Freund’s adjuvant (CFA)-induced adjuvant arthritis (AA) rat model results in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group.
Animal Model: | Freund’s adjuvant (CFA)-induced adjuvant arthritis (AA) rat model. |
Dosage: | 5 and 20 mg/kg |
Administration: | Oral administration daily between day 10-20 postimmunization. |
Result: | Resulted in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group. |