Valsartan (CGP-48933) - Moligand™, 10mM in DMSO , Antagonist of AT 1 receptor, CAS No.137862-53-4, Antagonist of AT 1 receptor

CAS: 137862-53-4 Cat. No.: V408202 Molecular Weight: 435.52 EC Number: 604-045-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

N-​(1-​oxopentyl)​-​N-​[[2'-​(2H-​tetrazol-​5-​yl)​[1,​1'-​biphenyl]​-​4-​yl]​methyl]​-L-​valine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Valsartan (CGP-48933) Valsartan (CGP-48933) is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.
In vitro

Valsartan dose-dependently inhibits the vasoconstriction induced by angiotensin II and lowers blood pressure in renin-dependent models of hypertension. Valsartan is at least as effective as ACE inhibitors, diuretics, beta-blockers and calcium antagonists.

In vivo

Valsartan results in improved glucose tolerance, reduced fasting blood glucose levels, and reduced serum insulin levels in mice fed a Western diet. Valsartan treatment also blocks Western diet-induced increases in serum levels of the proinflammatory cytokines interferon-gamma and monocyte chemotactic protein 1. Valsartan enhances mitochondrial function and prevents Western diet-induced decreases in glucose-stimulated insulin secretion in the pancreatic islets of mice. Valsartan treatment blocks or attenuates Western diet-induced changes in expression of several key inflammatory signals: interleukin 12p40, interleukin 12p35, tumor necrosis factor-alpha, interferon-gamma, adiponectin, platelet 12-lipoxygenase, collagen 6, inducible NO synthase, and AT1R in isolated adipocytes. Valsartan significantly increases insulin-mediated 2-[3H]deoxy-d-glucose (2-[3H]DG) uptake into skeletal muscle and attenuates the increase in plasma glucose concentration after a glucose load and plasma concentrations of glucose and insulin. Valsartan treatment exaggerates the insulin-induced phosphorylation of IRS-1, the association of IRS-1 with the p85 regulatory subunit of phosphoinositide 3 kinase (PI 3-K), PI 3-K activity, and translocation of GLUT4 to the plasma membrane. Valsartan also reduces tumor necrosis factor-alpha (TNF-alpha) expression and superoxide production in skeletal muscle of KK-Ay mice.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

N-​(1-​oxopentyl)​-​N-​[[2'-​(2H-​tetrazol-​5-​yl)​[1, ​1'-​biphenyl]​-​4-​yl]​methyl]​-L-​valine

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Valsartan (CGP-48933) is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Antagonist of AT 1 receptor

Product Properties

• ALogP: 4.4

Names and Identifiers

• Isomeric SMILES: CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)[C@@H](C(C)C)C(=O)O
• WGK Germany: 3
• Alternate CAS: 137862-53-4
• NSC Number: 758927
• MeSH Entry Terms: 48933, CGP;CGP 48933;Diovan;Kalpress;Miten;N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine;Nisis;Provas;Tareg;Vals;valsartan
• Molecular Weight: 435.52
• Reaxy-Rn: 24721853
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24721853&ln=

Associated Targets(Human)

AGTR1 Tclin Type-1 angiotensin II receptor (1 Activities)

Discover Target: AGTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Specific Rotation[α]: -65°C
• Melt Point(°C): 117°C

References

1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo.  (2023)  Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection.  JOURNAL OF FOOD COMPOSITION AND ANALYSIS,      [PMID:] [10.1016/j.jfca.2023.105825]

2. Huimin Zhou, Zhiwei Qiu, Jin Zeng, Ruobin Dai, Zhiwei Wang.  (2023)  Ultra-permeable polyamide nanofiltration membrane modified by hydrophilic-hydrophobic alternated lignocellulosic nanofibrils for efficient water reuse.  JOURNAL OF MEMBRANE SCIENCE,      [PMID:] [10.1016/j.memsci.2023.122125]

3. Zhiren Zou, Qiang Huang, Xiaobo Li, Xianzhi Liu, Lina Yin, Yunjie Zhao, Guang Liang, Wenqi Wu.  (2023)  Dissolution changes in drug-amino acid/biotin co-amorphous systems: Decreased/increased dissolution during storage without recrystallization.  EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES,      [PMID:37442486] [10.1016/j.ejps.2023.106526]

4. Mingkang Zhang, Ruirui Cui, Yan Zhou, Yanrong Ma, Yongwen Jin, Lina Wang, Wen Kou, Xin’an Wu.  (2023)  Accumulation of Renal Fibrosis in Hyperuricemia Rats Is Attributed to the Recruitment of Mast Cells, Activation of the TGF-β1/Smad2/3 Pathway, and Aggravation of Oxidative Stress.  INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,  24  (13): (10839).  [PMID:37446016] [10.3390/ijms241310839]

5. Yupeng Shi, Mengyang Zhou, Shuo Zhao, Haotian Li, Wenhao Wang, Jingliang Cheng, Lin Jin, Yifei Wang.  (2023)  Janus amphiphilic nanofiber membranes synergistically drive antibacterial and anti-inflammatory strategies for skin wound healing.  MATERIALS & DESIGN,      [PMID:] [10.1016/j.matdes.2023.111778]

6. Qiang Huang, Zhiren Zou, Xiaobo Li, Qinwen Xiao, Guang Liang, Wenqi Wu.  (2023)  Poly (amino acid)s as new co-formers in amorphous solid dispersion.  INTERNATIONAL JOURNAL OF PHARMACEUTICS,      [PMID:36706970] [10.1016/j.ijpharm.2023.122645]

7. Mingkang Zhang, Ruirui Cui, Yan Zhou, Yanrong Ma, Yongwen Jin, Xueyan Gou, Jinru Yang, Xin’an Wu.  (2022)  Uric acid accumulation in the kidney triggers mast cell degranulation and aggravates renal oxidative stress.  TOXICOLOGY,      [PMID:36464070] [10.1016/j.tox.2022.153387]

8. Lin Chen, Li Ge, Qinghui Liang, Zhenbo Zhao, Kedi Yang.  (2022)  Eutectic solvents formed by (+)-DTTA and L-menthol as novel chiral recognition and separation media for enantioselective extraction of valsartan enantiomers.  JOURNAL OF MOLECULAR LIQUIDS,      [PMID:] [10.1016/j.molliq.2022.120818]

9. Ke Lin, Wu Luo, Na Yang, Lan Su, Hao Zhou, Xiang Hu, Yi Wang, Zia A. Khan, Weijian Huang, Gaojun Wu, Guang Liang.  (2022)  Inhibition of MyD88 attenuates angiotensin II-induced hypertensive kidney disease via regulating renal inflammation.  INTERNATIONAL IMMUNOPHARMACOLOGY,      [PMID:36116148] [10.1016/j.intimp.2022.109218]

10. Wang Yiran, Shi Jihua, Dai Dapeng, Cai Jianping, Wang Shuanghu, Hong Yun, Zhou Shan, Zhao Fangling, Zhou Quan, Geng Peiwu, Zhou Yunfang, Xu Xue, Luo Qingfeng.  (2022)  Evaluation of commonly used cardiovascular drugs in inhibiting vonoprazan metabolism in vitro and in vivo.  Frontiers in Pharmacology,      [PMID:36052128] [10.3389/fphar.2022.909168]

11. Yan Zhou, Mengmeng Wei, Mingkang Zhang, Jianping Zhang, Fabing Tang, Xin’an Wu.  (2022)  Adefovir accumulation in the renal interstitium triggers mast cell degranulation and promotes renal interstitial fibrosis.  TOXICOLOGY LETTERS,      [PMID:35114312] [10.1016/j.toxlet.2022.01.018]

12. Xiao Juan Liu, Yang Zhang, Xue Zhong Wang.  (2020)  Study on Co-Crystallization of LCZ696 Using In Situ ATR-FTIR and Imaging.  Crystals,  10  (10): (922).  [PMID:] [10.3390/cryst10100922]

13. Qi Liang, Xiaoying Fu, Jianfeng Zhang, Jiaxue Hao, Gangjun Feng, Jing Wang, Qian Li, Faizan Ahmad, Xinfeng Zhao.  (2020)  Immobilized angiotensin II type I receptor: A powerful method of high throughput screening for antihypertensive compound identification through binding interaction analysis.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:32156458] [10.1016/j.chroma.2020.461003]

14. Yi-Lin Sun, Peng-Hui Li, Ling Shi, Wan-Zhen Su, De-Sheng Li, Gen-Long Xue, Yue Zhao, Chang-Zhu Li, Ying Li, Yang Zhou, Shang-Xuan Li, Yang Zhang, Yan-Jie Lu, Zhen-Wei Pan.  (2018)  Valsartan reduced the vulnerability to atrial fibrillation by preventing action potential prolongation and conduction slowing in castrated male mice.  JOURNAL OF CARDIOVASCULAR ELECTROPHYSIOLOGY,  29  (10): (1436-1443).  [PMID:30016000] [10.1111/jce.13697]

15. Xiaohua Xu, Yongzhi Xu, Shengqiang Liang.  (2024)  Analytical Interference in Chemiluminescence Assay–Measured Angiotensin I, Angiotensin II, Aldosterone, and Renin.  JOURNAL OF CLINICAL LABORATORY ANALYSIS,  38  (10): (e25045).  [PMID:38822626] [10.1002/jcla.25045]

16. Jia-Huan He, Xiang-Jun Li, Shi-Peng Wang, Xia Guo, Hao-Xuan Chu, Han-Chi Xu, Yu-Shi Wang.  (2024)  Eugenol Inhibits Ox-LDL-Induced Proliferation and Migration of Human Vascular Smooth Muscle Cells by Inhibiting the Ang II/MFG-E8/MCP-1 Signaling Cascade.  Journal of Inflammation Research,      [PMID:38328560] [10.2147/JIR.S446960]

17. Huixiang Zhang, Yang Zhang, Fumin Xue, Hui Chen, Zhenguo Gao, Shichao Du, Yan Wang.  (2024)  Insight into the dissolution behavior of valsartan (form E) in twelve pure solvents: Solubility, modelling and molecular simulation.  JOURNAL OF MOLECULAR LIQUIDS,      [PMID:] [10.1016/j.molliq.2024.124774]

18. Wen Luo, Zhenzhen Li, Junjie Che, Xinyao Li, Huali Zhang, Jinxiu Tian, Chunyang Wang, GuiYing Li, Lin Jin.  (2024)  Near-Infrared Responsive Nanocomposite Hydrogel Dressing with Anti-Inflammation and Pro-Angiogenesis for Wound Healing.  ACS Applied Materials & Interfaces,      [PMID:38934381] [10.1021/acsami.4c06193]

19. Chenglin Liang, Ge Zhang, Linlin Guo, Xinyi Ding, Heng Yang, Hongling Zhang, Zhenzhong Zhang, Lin Hou.  (2024)  Spatiotemporal transformable nano-assembly for on-demand drug delivery to enhance anti-tumor immunotherapy.  Asian Journal of Pharmaceutical Sciences,      [PMID:38434719] [10.1016/j.ajps.2024.100888]

20. Detao Li, Wenqian Chen, Limin Zhou, Li Xu, Feiqiang He, Jerry Y Y Heng, Hamza Shehzad, Jinbo Ouyang.  (2024)  Uncovering Cocrystal Formation and Competition Mechanism of Polyhydroxy Natural Products: Cases of Quercetin, Hesperidin, Resveratrol, and Curcumin.  CRYSTAL GROWTH & DESIGN,      [PMID:] [10.1021/acs.cgd.4c00291]

21. Ramsha Khalid, Syed Mahmood, Zarif Mohamed Sofian, Zamri Chik, Yi Ge.  (2025)  Development of Rapidly Dissolving Microneedles Integrated with Valsartan-Loaded Nanoliposomes for Transdermal Drug Delivery: In Vitro and Ex Vivo Evaluation.  Pharmaceutics,  17  (4): (483).  [PMID:40284478] [10.3390/pharmaceutics17040483]

22. Fei Lingyan, Wang Honghong, Zhao Dongliang, Wang Xiaohua, Ren Jizhen, Liu Lanyun, Tang Chun, Lei Yan, Wang Qingqing, Nie Yuanpeng, Liu Yang, Li Na, Zhong Ming, Xu Nan, Wei Jin, Persson Pontus B., Patzak Andraes, Khedkar Pratik H., Zheng Zhihua, Jiang Shan.  (2025)  Rescuing vascular dysfunction in dorsal pancreatic arteries prevents tacrolimus-induced glucose metabolism disorder in mice.  MOLECULAR MEDICINE,  31  (1): (1-15).  [PMID:40495121] [10.1186/s10020-025-01282-7]

23. Rongrong Xue, Tuanjia Li, Yingying He, Fenghua Chen, Wang-Chuan Xiao.  (2026)  Supercooled Liquid during the Evaporation and Cooling Crystallization of Valsartan：A Macroscopic Observation.  CRYSTENGCOMM,      [PMID:] [10.1039/D5CE01019E]

24. Yunshan Wang, Nan Lu, Peiyao Wu, Yue Chu, Yonghao Xing, Jing Wang, Xinfeng Zhao.  (2026)  An Allosteric Assay for Identifying Ligands Binding to β2 Adrenergic Receptor by Surface-Enhanced Raman Scattering (SERS)-Active Nanoparticles.  ANALYTICAL CHEMISTRY,      [PMID:41637639] [10.1021/acs.analchem.5c07045]

25. Lingyan Fei, Xiaohua Wang, Lingyi Kong, Tianjiao Cui, Pratik H Khedkar, Yunxiu Xiang, Dongliang Zhao, Junxuan Fang, Yulin Liang, Yangyang Zhang, Nan Xu, Xingyu Qiu, Liang Zhao, Gensheng Zhang, Yan Lei, Chun Tang, Kongyang Ma, Liwei Lu, Jin Wei, En Yin Lai, Pontus B Persson, Andreas Patzak, Zhihua Zheng, Shan Jiang.  (2026)  Tacrolimus Induced Hypertension and Vascular Remodeling Includes Mechanisms of Cellular Senescence—The Protective Effect of Valsartan.  Acta Physiologica,  242  (4): (e70189).  [PMID:41814130] [10.1111/apha.70189]