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Valsartan

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Chemical Structure| 137862-53-4 同义名 : CGP 48933
CAS号 : 137862-53-4
货号 : A133780
分子式 : C24H29N5O3
纯度 : 95%
分子量 : 435.52
MDL号 : MFCD00865840
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(114.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AT2 receptor
描述 Valsartan is a blocker in angiotensin II receptor used in the treatment of hypertension and congestive heart failure, with IC50 ranging from 39.5 to116 uM. In vitro,Valsartan (50 μM) induced a significant increase in p-AMPK and p-LKB1.Valsartan inhibited NF - κ B activity and significantly reduced the expression and activity of inflammatory cytokines, TLR-4, TF induced by Hg[3]. The main antihypertensive effect of valsartan is mediated by a reduction in angiotensin II activation of the AT1-R in vascular smooth muscle. The peak plasma concentration (C max) of valsartan occurs within 2-4 h after dosing, and absolute bioavailability is roughly 25%[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00190580 Chronic Kidney Disease ... 展开 >> Hypertension 收起 << Phase 4 Completed - Japan ... 展开 >> St. Marianna University School of Medicine Kawasaki, Kanagawa, Japan, 216-8511 收起 <<
NCT00386607 Hypertension Phase 3 Completed - United States, California ... 展开 >> Investigative Centers San Diego, California, United States Canada Investigative Centers Canada, Canada Germany Investigative Centers Germany, Germany Netherlands Investigative Centers Netherlands, Netherlands 收起 <<
NCT00386607 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.48mL

2.30mL

1.15mL

22.96mL

4.59mL

2.30mL
参考文献

[1]Cole BK, Keller SR, et al. Valsartan protects pancreatic islets and adipose tissue from the inflammatory and metabolic consequences of a high-fat diet in mice. Hypertension. 2010 Mar;55(3):715-21.

[2]Chiolero A, Burnier M. Pharmacology of valsartan, an angiotensin II receptor antagonist. Expert Opin Investig Drugs. 1998 Nov;7(11):1915-25.

[3]Ha YM, Park EJ, Kang YJ, Park SW, Kim HJ, Chang KC. Valsartan independent of AT₁ receptor inhibits tissue factor, TLR-2 and -4 expression by regulation of Egr-1 through activation of AMPK in diabetic conditions. J Cell Mol Med. 2014 Oct;18(10):2031-43. doi: 10.1111/jcmm.12354. Epub 2014 Aug 11. PMID: 25109475; PMCID: PMC4244018.

[4]Giles TD, Cockcroft JR, Pitt B, Jakate A, Wright HM. Rationale for nebivolol/valsartan combination for hypertension: review of preclinical and clinical data. J Hypertens. 2017 Sep;35(9):1758-1767. doi: 10.1097/HJH.0000000000001412. PMID: 28509722; PMCID: PMC5548499.