Valsartan (Synonyms: CGP 48933) |
Catalog No.GC10765
One-Click Copy Product Info
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Valsartan is a nonpeptide angiotensin receptor antagonist that selectively blocks the binding of angiotensin II to the angiotensin II type 1 receptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 137862-53-4
Sample solution is provided at 25 µL, 10mM.
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Valsartan is a nonpeptide angiotensin receptor antagonist that selectively blocks the binding of angiotensin II to the angiotensin II type 1 receptor[1]. Valsartan improves cardiac remodeling by inhibiting guanine nucleotide-binding proteins and blocking EGFR activation, and contributes to the synergistic effects mediated downstream of Sacubitril via its regulation of glycogen synthase kinase-3 beta (GSK3B) and the activities of the segment polarity protein disheveled homologs DVL-1, 2, and 3[2]. Valsartan has been widely used in immune response studies to inhibit the production of reactive oxygen species (ROS) as well as the binding activity of NF-κB, and to regulate inflammation[3].
In vitro, Valsartan treatment (1μM) for 48 hours inhibited the expression of MCP-1 and TGF-β1 in rat glomerular mesangial cells (GMCs) and glomerular epithelial cells (GECs) induced by high glucose, and alleviated oxidative stress[4]. Incubation of BEAS-2B cells with 80μM Valsartan for 24 hours alleviated the decrease in cell viability triggered by 50μg/ml lipopolysaccharide (LPS), suppressed the expression of MUC5AC at both transcriptional and translational levels, and blocked the phosphorylation of p65, p38, ERK and JNK[5].
In vivo, Valsartan treatment via oral administration at a dose of 40mg/kg/day for 18 days reduced tumor volume and weight, and restrained angiogenesis in a mouse model of colorectal cancer[6]. Oral administration of Valsartan at a dose of 10mg/kg/day for 2 weeks reduced infarct size and cardiomyocyte apoptosis, and decreased plasma TNF-α levels in a rat model of myocardial ischemia-reperfusion injury[7]. Oral administration of Valsartan at a dose of 10mg/kg/day for 5 months lowered brain β-amyloid levels and improved spatial learning ability in a mouse model of Alzheimer's disease[8].
References:
[1] Black H R, Bailey J, Zappe D, et al. Valsartan: more than a decade of experience[J]. Drugs, 2009, 69(17): 2393-2414.
[2] Iborra-Egea O, Gálvez-Montón C, Roura S, et al. Mechanisms of action of sacubitril/valsartan on cardiac remodeling: a systems biology approach[J]. NPJ systems biology and applications, 2017, 3(1): 12.
[3] Dandona P, Kumar V, Aljada A, et al. Angiotensin II receptor blocker valsartan suppresses reactive oxygen species generation in leukocytes, nuclear factor-κB, in mononuclear cells of normal subjects: evidence of an antiinflammatory action[J]. The Journal of Clinical Endocrinology & Metabolism, 2003, 88(9): 4496-4501.
[4] Jiao B, Wang Y, Cheng Y, et al. Valsartan attenuated oxidative stress, decreased MCP-1 and TGF-β1 expression in glomerular mesangial and epithelial cells induced by high-glucose levels[J]. BioScience Trends, 2011, 5(4): 173-181.
[5] Zhou M, Meng L, He Q, et al. Valsartan attenuates LPS-induced ALI by modulating NF-κB and MAPK pathways[J]. Frontiers in pharmacology, 2024, 15: 1321095.
[6] Asgharzadeh F, Mostafapour A, Ebrahimi S, et al. Inhibition of angiotensin pathway via valsartan reduces tumor growth in models of colorectal cancer[J]. Toxicology and Applied Pharmacology, 2022, 440: 115951.
[7] Wu B, Lin R, Dai R, et al. Valsartan attenuates oxidative stress and NF-κB activation and reduces myocardial apoptosis after ischemia and reperfusion[J]. European journal of pharmacology, 2013, 705(1-3): 140-147.
[8] Wang J, Ho L, Chen L, et al. Valsartan lowers brain β-amyloid protein levels and improves spatial learning in a mouse model of Alzheimer disease[J]. The Journal of clinical investigation, 2007, 117(11): 3393-3402.
| Cell experiment [1]: | |
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Cell lines |
BEAS-2B cells |
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Preparation Method |
BEAS-2B cells were RPMI-1640 medium supplemented with 100μg/ml streptomycin, 100μg/ml penicillin and 10% fetal bovine serum at 37°C in an incubator with 5% CO2. BEAS-2B cells (5×103/well) were seeded in the 96-well plates and cultured for 12h before 24h-starvation followed by treatment with different concentrations of Valsartan (0, 20, 40, and 80µM) in the presence of LPS (50μg/ml) for 24h. Cells were then washed twice with sterile PBS and the viability was measured. |
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Reaction Conditions |
0, 20, 40, and 80µM; 24h |
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Applications |
Valsartan restored the LPS-treated cell viability in BEAS-2B cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
BALB/c mice |
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Preparation Method |
BALB/c mice, aged 7 weeks with weights of 22-25g, were housed in cages and maintained in air-conditioned animal quarters with a 12h light-dark cycle and free access to autoclaved tap water and a standard chow diet. 2×106 CT-26 cells were injected in the right flank region of mouse and approximately two weeks, when tumors reached a volume of 80-100mm3, mice were separated into four groups randomly as below: (1) Control (Untreated mice), (2) Valsartan (treated with 40mg/kg/day; orally; 18 days). The size of tumor was assessed every other day with the digital caliper. |
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Dosage form |
40mg/kg/day; 18 days; p.o. |
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Applications |
Valsartan treatment reduced tumor growth in mice with CT-26 xenografts. |
References: [1] Zhou M, Meng L, He Q, et al. Valsartan attenuates LPS-induced ALI by modulating NF-κB and MAPK pathways[J]. Frontiers in pharmacology, 2024, 15: 1321095. [2] Asgharzadeh F, Mostafapour A, Ebrahimi S, et al. Inhibition of angiotensin pathway via valsartan reduces tumor growth in models of colorectal cancer[J]. Toxicology and Applied Pharmacology, 2022, 440: 115951. | |
| Cas No. | 137862-53-4 | SDF | |
| Synonyms | CGP 48933 | ||
| Chemical Name | (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid | ||
| Canonical SMILES | CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)C(C(C)C)C(=O)O | ||
| Formula | C24H29N5O3 | M.Wt | 435.52 |
| Solubility | ≥ 19.65mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2961 mL | 11.4805 mL | 22.9611 mL |
| 5 mM | 459.2 μL | 2.2961 mL | 4.5922 mL |
| 10 mM | 229.6 μL | 1.1481 mL | 2.2961 mL |
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)