Valsartan-CGP-48933-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEValsartanCat. No.: HY-18204CAS No.: 137862-53-4Synonyms: CGP 48933分式: CHNO分量: 435.52作靶点: Angiotensin Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (22

2、9.61 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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，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

3、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 (5.74 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 (5.74 mM); Clear solution1/3 Master of Small Molecules 您

4、边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.74 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Valsarta (CGP-48933)于治疗压和衰竭的管紧张素II受体拮抗剂。体外研究 Valsartan is a synthetic non-peptide angiotensin II type 1 receptor antagonist that dilates blood vessels andreduces blood pressure

5、by blocking the action of angiotensin. Valsartan significantly decreases theexpression of AT1R in ageing aorta endothelial cells 1. The pretreatment of valsartan results in an inhibitionof TLR2 signaling and proinflammatory cytokines. The expression of AGTR1 is up-regulated after alcoholexposure, an

6、d is blocked by valsartan pretreatment 2.体内研究 Valsartan significantly attenuates the expression of TGF-/Smad, Hif-1 and fibrosis-related protein in ratsafter MI. Heart function, infarcted size, wall thickness as well as myocardial vascularization of ischaemichearts are also significantly improved by

7、 valsartan compared with saline and hydralazine 3. Valsartanpartially reverses the effects of high-salt diet on hypertension, cardiac injuries such as fibrosis andinflammatory cell infiltration, and inhibition of aquaporin 1 and angiogenic factors; valsartan alone does notexert such effects 4. Valsa

8、rtan is an effective antidepressant/antianxiety reagent and can promote thehippocampal neurogenesis and expression of BDNF. Chronic administration of valsartan (5-40 mg/kg/d, p.o.)increases the time spent in the center of the field in OFT and the latency to eat in NSF, reduces theimmobility time in

9、both TST and FST, and increases the sucrose preference in SPT 5.PROTOCOLAnimal Rats: Rats are randomly divided into two groups: (i) valsartan-treated group that is given intravenously 3Administration 4 mg/kg/day valsartan in 0.5 mL normal saline via the vein daily for 1 week; (ii) hydralazine-treate

10、d groupreceiving 0.2 mg/kg/day hydralazine injection in saline; and (iii) control group that receives saline injection inthe same way (n=15 for each group) 4.Mice: Valsartan is dissolved in water containing 0.5% methylcellulose solution. Valsartan (5-40 mg/kg/d) isadministered by oral (p.o.) route i

11、n 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 commercialblood pressure analysis systemdesigned. The mice are trained for at least 2 consecutive days to adapt to theapparatus befo

12、re the study is initiated. To record the blood pressure, the mice are placed on a heated pad(35C) and measured with a programmable tail-cuff sphygmomanometer in steady state. The average of 10readings from each mouse is recorded 5.MCE has not independently confirmed the accuracy of these methods. Th

13、ey are for reference only.REFERENCES1. Shan H, et al. Valsartan ameliorates ageing-induced aorta degeneration via angiotensin II type 1 receptor-mediated ERK activity. J CellMol Med. 2014 Jun;18(6):1071-80.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. Wang Y, et al. Valsartan blocked alcohol-i

14、nduced, Toll-like receptor 2 signaling-mediated inflammation in human vascular endothelialcells. Alcohol Clin Exp 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 aftermyocardial infarcti

15、on. J Cell Mol Med. 2015 Aug;19(8):1773-82.4. Jiang Y, et al. Cardioprotective effect of valsartan in mice with short-term high-salt diet by regulating cardiac aquaporin 1 and angiogenicfactor expression. 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 BDNFprotein in unpredictable chronic mild stress mice. Pharmacol B