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/ Valsartan/缬沙坦

Valsartan/缬沙坦 {[allProObj[0].p_purity_real_show]}

货号：A133780 同义名： CGP 48933

Valsartan是一种选择性的血管紧张素 II AT1 受体拮抗剂，半衰期为 6 小时。

Valsartan/缬沙坦 化学结构 CAS号：137862-53-4
Valsartan/缬沙坦 化学结构
CAS号：137862-53-4
Valsartan/缬沙坦 3D分子结构
CAS号：137862-53-4
Valsartan/缬沙坦 化学结构 CAS号：137862-53-4
Valsartan/缬沙坦 3D分子结构 CAS号：137862-53-4
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Valsartan/缬沙坦 纯度/质量文件 产品仅供科研

货号：A133780 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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Valsartan/缬沙坦 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].

Valsartan/缬沙坦 细胞实验

Cell Line
Concentration Treated Time Description References
AML-12 cells 20µM 12 hours To investigate the effect of Sac/Val on FGF21 expression in AML-12 cells, results showed that Sac/Val upregulated FGF21 expression via PPARα Cardiovasc Diabetol. 2025 Feb 22;24(1):89.
H9C2 cells 20µM 12 hours To investigate the effect of Sac/Val on FGF21 expression in H9C2 cells under hypoxic conditions, results showed that Sac/Val significantly upregulated FGF21 expression Cardiovasc Diabetol. 2025 Feb 22;24(1):89.
NIH-3T3 cells (induced as CAFs) 5 μg/ml Val and 0.5 μg/ml DOX 72 hours Regulate CAFs activity and reduce collagen expression Asian J Pharm Sci. 2024 Feb;19(1):100888.
4T1 tumor cells 5 μg/ml Val and 0.5 μg/ml DOX 72 hours Induce tumor cell senescence and inhibit proliferation and migration Asian J Pharm Sci. 2024 Feb;19(1):100888.
Human aortic endothelial cells (HAECs) 10 μM Valsartan + 15–240 μg/mL IS 18 hours Valsartan significantly increased nitrite levels in HAECs, while IS at 60–240 μg/mL significantly decreased valsartan-induced nitrite production in a dose-dependent manner. Redox Biol. 2020 Feb;30:101433.
Primary cortico-hippocampal neurons 100 μM 24 hours Inhibited oligomerization of Aβ1–42 into high-molecular-weight (HMW) soluble oligomers J Clin Invest. 2007 Nov;117(11):3393-402.

Valsartan/缬沙坦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Subtotal nephrectomy (SNx) mice Oral (Valsartan) and intraperitoneal (IS) 60 mg/kg/day Valsartan daily, IS thrice a week for six weeks Valsartan significantly improved blood flow reperfusion and CD31+ capillary density in ischemic limbs of SNx mice, while IS attenuated the protective effect of valsartan. Cotreatment with apocynin and calphostin C reversed the IS-mediated inhibition of valsartan-induced neovascularization. Redox Biol. 2020 Feb;30:101433.
Transgenic TG(mRen2)27(Ren2) rats Hypertension and non-alcoholic fatty liver disease model Oral 30 mg/kg/day Once daily for 3 weeks To evaluate the effects of valsartan on hypertension and non-alcoholic fatty liver disease. Results showed that valsartan significantly attenuated hepatic oxidative stress, steatosis, inflammation, and fibrosis. J Hepatol. 2008 Sep;49(3):417-28
Mice Myocardial infarction model Oral gavage 52 mg/kg/day Once daily for 14 days To investigate the effect of Sac/Val on cardiac function, fibrosis, and oxidative stress in MI mice, results showed that Sac/Val improved cardiac function and reduced fibrosis and oxidative stress by upregulating FGF21 expression Cardiovasc Diabetol. 2025 Feb 22;24(1):89.
Mice Tg2576 AD model mice Oral administration via drinking water 10 or 40 mg/kg/d Approximately 5 months of continuous treatment Reduced brain HMW Aβ oligomers, improved spatial learning deficits, and attenuated amyloid plaque pathology J Clin Invest. 2007 Nov;117(11):3393-402.
BALB/c mice 4T1 tumor model Intravenous injection 40 mg/kg Dosing interval not specified, continued until tumor volume endpoint Significantly inhibits tumor growth and lung metastasis, extends survival Asian J Pharm Sci. 2024 Feb;19(1):100888.
Transgenic Ren2 rats Transgenic Ren2 rat model Intraperitoneal injection 30 mg/kg/day Once daily for 21 days To evaluate the effects of Valsartan on myocardial hypertrophy and fibrosis in transgenic Ren2 rats. Results showed that Valsartan significantly reduced systolic blood pressure and serum aldosterone levels, and improved markers of myocardial hypertrophy and fibrosis. Metabolism. 2013 Jun;62(6):861-72
Mice High-fat diet-induced type 2 diabetes model and db/db mice model Drinking water 10 mg/kg/day Once daily for 8 weeks To investigate the effects of valsartan alone or in combination with vildagliptin in a mouse model of type 2 diabetes. Results showed that combination therapy significantly improved glucose metabolism, insulin sensitivity, reduced inflammatory markers, and ameliorated hepatic steatosis and pancreatic beta-cell function. Cardiovasc Diabetol. 2013 Nov 4;12:160
C57BL/6J mice Experimental acute myocardial infarction model Oral gavage 20 mg/kg BW/day Once daily for 28 days To investigate the effect of LCZ696 on cardiac rupture and survival rate after acute myocardial infarction. Results showed that LCZ696 significantly reduced the incidence of cardiac rupture and improved survival rate. JACC Basic Transl Sci. 2017 Dec 25;2(6):655-668
Mice Diabetic cardiomyopathy model Subcutaneous osmotic minipumps 2 mg/kg Replaced every 4 weeks for 10 weeks Prevented diabetes-induced cardiac dysfunction, reduced oxidative stress and cardiomyocyte apoptosis Cardiovasc Diabetol. 2013 Nov 12;12:169

Valsartan/缬沙坦 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 - -

Valsartan/缬沙坦 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.

Valsartan/缬沙坦 实验方案

计算器
存储液制备 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

Valsartan/缬沙坦 技术信息

CAS号137862-53-4
分子式C24H29N5O3
分子量 435.52
SMILES Code CC(C)[C@H](N(CC1=CC=C(C2=CC=CC=C2C3=NN=NN3)C=C1)C(CCCC)=O)C(O)=O
MDL No. MFCD00865840
别名 CGP 48933
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Valsartan | CGP 48933 | Cardiovascular System | Drug Standard | Depressurization | Angiotensin Receptor | AmBeed-信号通路专用抑制剂 | Valsartan/缬沙坦 纯度/质量文件 | Valsartan/缬沙坦 生物活性 | Valsartan/缬沙坦 临床数据 | Valsartan/缬沙坦 参考文献 | Valsartan/缬沙坦 实验方案 | Valsartan/缬沙坦 技术信息

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