中文名 | SB273005 |
英文名 | SB273005 |
别名 | 化合物SB273005 SB273005 INTEGRIN抑制剂 |
英文别名 | SB273005 [8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid 1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-8-[2-[6-(methylamino)-2-pyridinyl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-, (4S)- (S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid |
CAS | 205678-31-5 |
化学式 | C22H24F3N3O4 |
分子量 | 451.44 |
密度 | 1.321±0.06 g/cm3(Predicted) |
沸点 | 662.9±55.0 °C(Predicted) |
酸度系数 | 4.32±0.10(Predicted) |
存储条件 | -20℃ |
体外研究 | In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). 在体外,SB273005抑制人破骨细胞介导的骨吸收,IC50 为11 nM。在包含MDA-MB-231细胞的血液中,SB273005与lamifiban结合抑制肿瘤细胞粘附到血管细胞外基质上(ECM)。 |
体内研究 | In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. 在骨吸收和骨质疏松大鼠模型中,SB273005 (30 mg/kg, p.o.)抑制甲状旁腺素刺激的血钙反应,并抑制骨损失。在佐剂性关节炎大鼠体内,SB273005 (60 mg/kg, p.o.)显著减少佐剂诱导的关节炎症状。 在大鼠主动脉和肾动脉中,SB273005 (1000 mg/kg/day, p.o.)引起血管平滑肌细胞(VSMC)急性暂时性坏死。在怀孕的小鼠体内,SB273005逆转Th1细胞产生的IL-2 l水平的下降,以及Th2细胞衍生的IL-10水平的增加。 |
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