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编 号:F487656
分子式:C24H25N5O
分子量:399.49
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5mg
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10mg
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50mg
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100mg
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生物活性:
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).

体内研究:
Dorsomorphin (化合物 C:10 mg/kg,静脉注射一次) 处理导致总血清铁浓度增加 60%,降低成年小鼠铁调素表达的基础水平并增加血清铁浓度。 Dorsomorphin (化合物 C:0.2 mg/kg,静脉注射,LPS 注射前 30 分钟) 降低注射 LPS 的大鼠主动脉中的 ICAM-1 和 VCAM-1 表达。 Dorsomorphin (化合物 C;25 mg/kg;腹腔注射;在雄性 BALB/c 小鼠中) 在注射脂多糖 (LPS) 之前进行处理,与仅接受 LPS 处理的动物相比,显著降低了致死率。Animal Model:Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin.
Dosage:10 mg/kg.
Administration:Intravenously once.
Result:Led to a 60% increase in total serum iron concentrations.Effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice.
Animal Model:Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g).
Dosage:0.2 mg/kg.
Administration:I.V., 30 min before LPS injection.
Result:Reduced ICAM-1 and VCAM-1 expression in LPS-injected rat aorta.
Animal Model:Male BALB/c mice at 6-7 weeks of age weighing 20-22 g
Dosage:25 mg/kg
Administration:Injection i.p.; 60 min before LPS challenge
Result:Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only.

体外研究:
Dorsomorphin (compound C) (0-10 μM,18 h) 以剂量依赖性方式抑制人纤维肉瘤 HT1080 细胞中 2DG 诱导的 GRP78 启动子活性,但对衣霉素诱导的 GRP78 启动子活性几乎没有影响。Dorsomorphin (compound C) C 还抑制葡萄糖戒断诱导的 GRP78 启动子活性。Dorsomorphin (化合物 C) 对 2DG 诱导的 PERK 激活没有影响,并降低 HT1080 细胞中基础和 2DG 诱导的 AMPK 磷酸化水平。
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