野百合堿作用機制 - Medchemexpress - MCE中國

1、Product Data SheetMonocrotalineCat. No.: HY-N0750CAS No.: 315-22-0分式: CHNO分量: 325.36作靶點: Others作通路: Others儲存式: 4C, sealed storage, away from moisture and light* In solvent : -80C, 6 months; -20C, 1 month (sealed storage, away frommoisture and light)溶解性數(shù)據(jù)體外實驗 DMSO : 37.5 mg/mL (115.26 mM; Need ultras

2、onic)H2O : 4 mg/mL (12.29 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (sealed st

3、orage, away from moisture and light)。-80C儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% sa

4、lineSolubility: 2.5 mg/mL (7.68 mM); Clear solution此案可獲得 2.5 mg/mL (7.68 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.68 mM); Clear solution此案

5、可獲得 2.5 mg/mL (7.68 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.68 mM); Clear solution此案可獲得 2.5 mg/mL (7.68 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg

6、/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Monocrotaline從豬屎植物的種提取的吡咯西啶物堿，于在嚙齒動物中誘導(dǎo)肺動脈壓。體外研究 Monocrotaline (MCT) is an 11-membered macrocyclic pyrrolizidine alkaloid (PA) derived from the seeds of theCrotalaria spectabilis plant1. Monocrotaline a natural ligand exhibits dose-dependent cyt

7、otoxicity with potentantineoplastic activity. The in vitro cytotoxicity of monocrotaline is proved at IC50 24.966 g/mL and genotoxicity at 2X IC50 against HepG2 cells2.體內(nèi)研究 MCT causes a pulmonary vascular syndrome in rats characterized by proliferative pulmonary vasculitis, pulmonaryhypertension (PH

8、), and cor pulmonale3. Among preclinical models of pulmonary arterial hypertension (PAH),monocrotaline animal model offers the advantage of mimic several key aspects of human PAH, including vascularremodeling, proliferation of smooth muscle cells, endothelial dysfunction, upregulation of inflammator

9、y cytokines,and right ventricle failure, requiring a single drug injection4. Changes in multiple pathways associated with thedevelopment of PH, including activated glycolysis, increased markers of proliferation, disruptions in carnitinehomeostasis, increased inflammatory and fibrosis biomarkers, and

10、 a reduction in glutathione biosynthesis areobserved with the injection of monocrotaline5.PROTOCOLAnimal Rats: A total of 20 male Sprague Dawley rats (SD; 220-270g) are used in this study (n=10 per group). Control groupAdministration 5 received vehicle for monocrotaline (MCT). Pre-pulmonary hyperten

11、sion (PH) group received a single injection of MCT(60 mg/kg i.p.) to induce and are sacrificed after 14 days5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Nat Commun. 2019 Aug 7;10(1):3551. J Cell Physiol. 2019 Oct 21. Toxicol Appl Pharma

12、col. 2019 Nov 14:114827.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Gomez-Arroyo JG, et al. The monocrotaline model of pulmonary hypertension in perspective. Am J Physiol Lung Cell Mol Physiol. 2012 FebPage 2 of 3 www.MedChemE15;302(4):L363-9.2. Kusuma SS, et al.

13、 Antineoplastic 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 animal model for the study of pulmonary arterial hypertension: A network approach. PulmPharmacol 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 Mar3;11(3):e0150480.McePdfHeightC