Monocrotaline-Crotaline-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMonocrotalineCat. No.: HY-N0750CAS No.: 315-22-0Synonyms: Crotaline分式: CHNO分量: 325.36作靶点: Others作通路: Others储存式: 4C, sealed storage, away from moisture and light* In solvent : -80C, 6 months; -20C, 1 month (sealedstorage, away fr

2、om moisture and light)溶解性数据体外实验 DMSO : 37.5 mg/mL (115.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0735 mL 15.3676 mL 30.7352 mL5 mM 0.6147 mL 3.0735 mL 6.1470 mL10 mM 0.3074 mL 1.5368 mL 3.0735 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，

3、配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.68 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.68 mM); Clear solution

4、3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.68 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Monocrotaline从猪屎植物的种提取的吡咯西啶物碱，于在啮齿动物中诱导肺动脉压。体外研究 Monocrotaline (MCT) is an 11-membered macrocyclic pyrrolizidine alkaloid (PA) derived from the se

5、eds ofthe Crotalaria spectabilis plant 1. Monocrotaline a natural ligand exhibits dose-dependent cytotoxicity withpotent antineoplastic activity. The in vitro cytotoxicity of monocrotaline is proved at IC50 24.966 g/mL andgenotoxicity at 2 X IC50 against HepG2 cells 2.体内研究 MCT causes a pulmonary vas

6、cular syndrome in rats characterized by proliferative pulmonary vasculitis,pulmonary hypertension (PH), and cor pulmonale 3. Among preclinical models of pulmonary arterialhypertension (PAH), monocrotaline animal model offers the advantage of mimic several key aspects ofhuman PAH, including vascular

7、remodeling, proliferation of smooth muscle cells, endothelial dysfunction,upregulation of inflammatory cytokines, and right ventricle failure, requiring a single drug injection 4.Changes in multiple pathways associated with the development of PH, including activated glycolysis,increased markers of p

8、roliferation, disruptions in carnitine homeostasis, increased inflammatory and fibrosisbiomarkers, and a reduction in glutathione biosynthesis are observed with the injection of monocrotaline 5.PROTOCOLAnimal Rats: A total of 20 male Sprague Dawley rats (SD; 220-270g) are used in this study (n=10 pe

9、r group). ControlAdministration 5 group received vehicle for monocrotaline (MCT). Pre-pulmonary hypertension (PH) group received a singleinjection of MCT (60 mg/kg i.p.) to induce and are sacrificed after 14 days 5.MCE has not independently confirmed the accuracy of these methods. They are for refer

10、ence only.户使本产品发表的科研献 Nat Commun. 2019 Aug 7;10(1):3551.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Gomez-Arroyo JG, et al. The monocrotaline model of pulmonary hypertension in perspective. Am J Physiol Lung Cell Mol Physiol. 2012Feb 15;302(4):L363-9.2. Kusuma SS, et al. An

11、tineoplastic activity of monocrotaline against hepatocellular carcinoma. Anticancer Agents Med Chem.2014;14(9):1237-48.3. Wilson DW, et, al. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992;22(5-6):307-25.4. Nogueira-Ferreira R, et al. Exploring the monocrotaline

12、animal model for the study of pulmonary arterial hypertension: A networkapproach. Pulm Pharmacol Ther. 2015 Dec;35:8-16.5. Rafikova O,et al. Metabolic Changes Precede the Development of Pulmonary Hypertension in the Monocrotaline Exposed RatLung.PLoS One. 2016 Mar 3;11(3):e0150480.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCaution: