中文名 | AG-1295 |
英文名 | AG-1295 |
别名 | 6,7-二甲基-2-苯基喹噁啉 酪氨酸磷酸化抑制剂AG1295 6,7-二甲基-2-苯基喹喔啉 |
英文别名 | AG 1295 AG-1295 TYROPHOSTIN AG1295 TYRPHOSTIN AG 1295 AG-1295 (NSC 380341 AG 1295 PLATELET-DERIVED GROW 6,7-DIMETHYL-2-PHENYLQUINOXALINE Quinoxaline, 6,7-dimethyl-2-phenyl- |
CAS | 71897-07-9 |
化学式 | C16H14N2 |
分子量 | 234.3 |
密度 | 1.127±0.06 g/cm3(Predicted) |
熔点 | 121 °C |
沸点 | 398.3±37.0 °C(Predicted) |
溶解度 | 氯仿 (微溶),乙酸乙酯 (微溶) |
酸度系数 | 1.29±0.30(Predicted) |
存储条件 | −20°C |
外观 | 白色固体 |
颜色 | Yellow |
体外研究 | AG 1295 inhibits PDGFR autophosphorylation with IC 50 s of 0.3-0.5 μM and 0.5-1 μM for membrane autophosphorylation assays and Swiss 3T3 cells, respectively. AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro. Cell Viability Assay Cell Line: Rabbit conjunctival fibroblasts cells Concentration: 1 μM, 10 μM, 100 μM Incubation Time: 3 days Result: Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB. |
体内研究 | AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibition of PDGFR-beta-triggered tyrosine phosphorylation. AG1295 (12 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces interstitial fibrosis as verified by a smaller Sirius-Red stained area and also by a reduced number of macrophages, and by the ED-A+ fibronectin deposition and the number of cells positive for alpha-smooth muscle actin. Animal Model: Sprague-Dawley rats (240-270 g) Dosage: 12 mg/kg Administration: Intraperitoneal injection; daily; for 14 or 21 days Result: Attenuated interstitial fibrosis in rat kidney after unilateral obstruction. |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 3 |
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