纈沙坦作用機制 - Medchemexpress - MCE中國

1、Product Data SheetValsartanCat. No.: HY-18204CAS No.: 137862-53-4分式: CHNO分量: 435.52作靶點: Angiotensin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg/mL (229.61 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 m

2、gConcentration制備儲備液1 mM 2.2961 mL 11.4805 mL 22.9611 mL5 mM 0.4592 mL 2.2961 mL 4.5922 mL10 mM 0.2296 mL 1.1481 mL 2.2961 mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro

3、 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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% salineSolubility: 2.5 mg/mL (5.74 mM); Clear solution此案可獲得 2.5 mg/mL (5.74 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/

4、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 (5.74 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.74 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 900 L 20% 的

5、SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.74 mM); Clear solution此案可獲得 2.5 mg/mL (5.74 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/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Valsarta (CGP-48933)于治療壓和衰竭的管緊張素II受體拮抗劑。體外研究 Valsartan is a s

6、ynthetic non-peptide angiotensin II type 1 receptor antagonist that dilates blood vessels and reducesblood pressure by blocking the action of angiotensin. Valsartan significantly decreases the expression of AT1R inageing aorta endothelial cells1. The pretreatment of valsartan results in an inhibitio

7、n of TLR2 signaling andproinflammatory cytokines. The expression of AGTR1 is up-regulated after alcohol exposure, and is blocked byvalsartan pretreatment2.體內研究 Valsartan significantly attenuates the expression of TGF-/Smad, Hif-1 and fibrosis-related protein in rats after MI.Heart function, infarcte

8、d size, wall thickness as well as myocardial vascularization of ischaemic hearts are also significantly improved by valsartan compared with saline and hydralazine3. Valsartan partially reverses the effects ofhigh-salt diet on hypertension, cardiac injuries such as fibrosis and inflammatory cell infi

9、ltration, and inhibition ofaquaporin 1 and angiogenic factors; valsartan alone does not exert such effects4. Valsartan is an effectiveantidepressant/antianxiety reagent and can promote the hippocampal neurogenesis and expression of BDNF. Chronicadministration of valsartan (5-40 mg/kg/d, p.o.) increa

10、ses the time spent in the center of the field in OFT and thelatency to eat in NSF, reduces the immobility time in both TST and FST, and increases the sucrose preference in SPT5.PROTOCOLAnimal Rats: Rats are randomly divided into two groups: (i) valsartan-treated group that is given intravenously 3 m

11、g/kg/dayAdministration 4 valsartan in 0.5 mL normal saline via the vein daily for 1 week; (ii) hydralazine-treated group receiving 0.2 mg/kg/dayhydralazine injection in saline; and (iii) control group that receives saline injection in the same way (n=15 for eachgroup)4.Mice: Valsartan is dissolved i

12、n water containing 0.5% methylcellulose solution. Valsartan (5-40 mg/kg/d) isadministered by oral (p.o.) route in a volume of 10 mL/kg body weight using the gavage technique. Potentialalteration in blood pressure in response to chronic treatment with valsartan is assessed with a commercial bloodpres

13、sure analysis systemdesigned. The mice are trained for at least 2 consecutive days to adapt to the apparatusbefore the study is initiated. To record the blood pressure, the mice are placed on a heated pad (35C) and measuredwith a programmable tail-cuff sphygmomanometer in steady state. The average o

14、f 10 readings from each mouse isrecorded5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻Page 2 of 3 www.MedChemE Drug Des Devel Ther. 2020 Feb 13;14:603-611. Eur J Pharmacol. 2020 Apr.See more customer validations on HYPERLINK www.MedChemE

15、www.MedChemEREFERENCES1. Shan H, et al. Valsartan ameliorates ageing-induced aorta degeneration via angiotensin II type 1 receptor-mediated ERK activity. J Cell Mol Med. 2014Jun;18(6):1071-80.2. Wang Y, et al. Valsartan blocked alcohol-induced, Toll-like receptor 2 signaling-mediated inflammation in

16、 human vascular endothelial cells. Alcohol ClinExp Res. 2014 Oct;38(10):2529-40.3. Sui X, et al. Novel mechanism of cardiac protection by valsartan: synergetic roles of TGF-1 and HIF-1 in Ang II-mediated fibrosis after myocardialinfarction. J Cell Mol Med. 2015 Aug;19(8):1773-82.4. Jiang Y, et al. C

17、ardioprotective effect of valsartan in mice with short-term high-salt diet by regulating cardiac aquaporin 1 and angiogenic factorexpression. Cardiovasc Pathol. 2015 Jul-Aug;24(4):224-9.5. Ping G, et al. Valsartan reverses depressive/anxiety-like behavior and induces hippocampal neurogenesis and expression of BDNF protein inunpredictable chronic mild stress mice. Phar