野百合碱 T2803

Product Introduction
Bioactivity


英文名: Monocrotaline

描述: Monocrotaline (Crotaline) 是一种吡咯里西啶生物碱，从猪屎豆植物的种子中提取得到，可诱导啮齿动物产生肺动脉高血压。

体外活性: Monocrotaline (MCT) is an 11-membered macrocyclic pyrrolizidine alkaloid (PA) derived from the seeds of the Crotalaria spectabilis plant[1]. Monocrotaline is a natural ligand that exhibits dose-dependent cytotoxicity with potent antineoplastic activity. The in vitro cytotoxicity of monocrotaline is proved at IC50 24.966 µg/mL and genotoxicity at 2 X IC50 against HepG2 cells[2].

体内活性: MCT leads to a pulmonary vascular syndrome in rats characterized by proliferative pulmonary vasculitis, pulmonary hypertension (PH), and cor pulmonale[3]. Among preClinicalal models of pulmonary arterial hypertension (PAH), monocrotaline animal model offers the advantage of mimic several key aspects of human PAH, including vascular remodeling, proliferation of smooth muscle cells, endothelial dysfunction, upregulation of inflammatory cytokines, and right ventricle failure, requiring a single drug injection[4]. Changes in many pathways associated with the development of PH, including activated glycolysis, increased markers of proliferation, disruptions in carnitine homeostasis, increased inflammatory and fibrosis biomarkers, and a reduction in glutathione biosynthesis are observed with the injection of monocrotaline[5].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (169.04 mM)


关键字: inhibit | Inhibitor | Monocrotaline

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