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Based on 23 publication(s) in Google Scholar
Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research.
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- 純度: 99.97%
- CAS 番号: 137862-53-4
- 分子式: C24H29N5O3
- 分子量:435.52
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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MedChemExpress（MCE）の使用を引用している文献 Valsartan
More- Nat Commun. 2024 Aug 27;15(1):7388. [Abstract]
- Nat Commun. 2023 Sep 21;14(1):5891. [Abstract]
- Cardiovasc Diabetol. 2025 Feb 22;24(1):89. [Abstract]
- Phytomedicine. 2023 Jun:114:154747. [Abstract]
- Clin Transl Med. 2023 Mar;13(3):e1213. [Abstract]
- Int J Mol Med. 2025 Feb;55(2):26. [Abstract]
- Chin Med. 2025 Aug 19;20(1):127. [Abstract]
- Drug Des Devel Ther. 2024 Dec 5:18:5641-5654. [Abstract]
- Drug Des Devel Ther. 2020 Feb 13;14:603-611. [Abstract]
- Int J Mol Sci. 2023 Feb 3;24(3):2960. [Abstract]
- Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
- Eur J Pharmacol. 2020 Aug 15;881:173120. [Abstract]
- Heliyon. 2023 Apr 10;9(4):e15270. [Abstract]
- Kaohsiung J Med Sci. 2025 Oct 17:e70127. [Abstract]
- Ren Fail. 2024 Dec;46(2):2392849. [Abstract]
- Arch Biochem Biophys. 2022 Nov 15:730:109415. [Abstract]
- Mol Biol Rep. 2026 Feb 26;53(1):434. [Abstract]
- J Cardiovasc Transl Res. 2022 Feb;15(1):131-142. [Abstract]
- Biomed Res Int. 2022 Jul 28:2022:5832543. [Abstract]
- Physiol Res. 2020 Jul 16;69(3):427-438. [Abstract]
- Chinese J Anal Chem. 2024 Oct.
- Research Square Preprint. 2023 Aug 3.
- Res Sq. 2023 Jul 17:rs.3.rs-3112163. [Abstract]
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Angiotensin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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AT1 Receptor |
Valsartan (CGP 48933) is a synthetic non-peptide angiotensin II type 1 receptor antagonist that dilates blood vessels and reduces blood pressure by blocking the action of angiotensin. Valsartan significantly decreases the expression of AT1R in ageing aorta endothelial cells[1].
The pretreatment of valsartan results in an inhibition of TLR2 signaling and proinflammatory cytokines. The expression of AGTR1 is up-regulated after alcohol exposure, and is blocked by valsartan pretreatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Valsartan partially reverses the effects of high-salt diet on hypertension, cardiac injuries such as fibrosis and inflammatory cell infiltration, and inhibition of aquaporin 1 and angiogenic factors; valsartan alone does not exert such effects[4].
Valsartan is an effective antidepressant/antianxiety reagent and can promote the hippocampal 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 the immobility time in both TST and FST, and increases the sucrose preference in SPT[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 137862-53-4
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性状 Solid
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分子量 435.52
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分子式 C24H29N5O3
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Color White to off-white
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SMILES
CC(C)[C@@H](C(O)=O)N(C(CCCC)=O)CC1=CC=C(C2=CC=CC=C2C3=NNN=N3)C=C1
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別名
Valsartan; CGP 48933
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (23)
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Journal Impact Factor
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Most Recent
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Nat Commun
The TGFβ type I receptor kinase inhibitor vactosertib in combination with pomalidomide in relapsed/refractory multiple myeloma: a phase 1b trial. [Abstract]2024 Aug 27;15(1):7388. PMID: 39191755 -
Nat Commun
Endothelial Sp1/Sp3 are essential to the effect of captopril on blood pressure in male mice. [Abstract]2023 Sep 21;14(1):5891. PMID: 37735515
Valsartan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 21;14(1):5891. [Abstract]
Mesenteric arteries from Ang II-induced hypertensive mice were respectively incubated in vehicle, captopril (10 μmol/L), lisinopril (10 μmol/L), ARB (Valsartan, 10 μmol/L), captopril with B1 blocker (1 μmol/L) and captopril with B2 blocker (1 μmol/L) for 6 h before measurement. Then, vascular reactivity of mesenteric resistance arteries to Ach with or without L-NAME pretreatment (10–4 mol/L, 30 min) and SNP.
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Cardiovasc Diabetol
Sacubitril/Valsartan partially alleviates myocardial infarction injury by activating the FGF21 signaling pathway via PPARs. [Abstract]2025 Feb 22;24(1):89. PMID: 39987117 -
Phytomedicine
Baicalin inhibits pressure overload-induced cardiac hypertrophy by regulating the SIRT3-dependent signaling pathway. [Abstract]2023 Jun:114:154747. PMID: 36931095
Valsartan purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Jun:114:154747. [Abstract]
The cardiomyocytes were preincubated with 12.5, 25, and 50 μM Baicalin or Valsartan (VAL; 0, 12.5, 25, 50 μM) for 1 h and then treated with 100 nM Ang II for 24 h. The mRNA ANF, BNP, and β-MHC were measured by Real-time PCR.
Valsartan purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Jun:114:154747. [Abstract]
The cardiomyocytes were preincubated with 12.5, 25, and 50 μM Baicalin or Valsartan (VAL; 0, 12.5, 25, 50 μM) for 1 h and then treated with 100 nM Ang II for 24 h. The protein expression of ANF, BNP, and β-MHC were measured by Western Blotting.
Valsartan purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Jun:114:154747. [Abstract]
The cardiomyocytes were preincubated with 12.5, 25, and 50 μM Baicalin or Valsartan (VAL; 0, 12.5, 25, 50 μM) for 1 h and then treated with 100 nM Ang II for 24 h.
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Clin Transl Med
Angiotensin receptor blockers retard the progression and fibrosis via inhibiting the viability of AGTR1+ CAFs in intrahepatic cholangiocarcinoma. [Abstract]2023 Mar;13(3):e1213. PMID: 36855786
Valsartan purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2023 Mar;13(3):e1213. [Abstract]
Cell viability results showed a different proliferation rate after administrating losartan (300 μM) or Valsartan (100 μM; 24, 48, 72 h) in CAFs #1, #2, #5 and #6 cells (CAFs #1–6 were isolated from iCCA tumour tissues).
Valsartan purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2023 Mar;13(3):e1213. [Abstract]
Gel contraction results of CAFs with losartan or Valsartan (100 μM; 8, 24, 48 h)administration at different time points. Left panel: contracted gel within black, green and purple lines represented DMSO, losartan, and valsartan, respectively. Right panel: quantification of gel contraction rate under losartan and valsartan.
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Int J Mol Med
Jinlida granules alleviate podocyte apoptosis and mitochondrial dysfunction via the AMPK/PGC‑1α pathway in diabetic nephropathy. [Abstract]2025 Feb;55(2):26. PMID: 39670303 -
Chin Med
Identification of anti-fibrotic compounds from Piper longum L via hollow fiber cell fishing and high-performance liquid chromatography with in vivo and in vitro validation. [Abstract]2025 Aug 19;20(1):127. PMID: 40830877 -
Drug Des Devel Ther
Integrating Metabolomics, Histopathology, and Cardiac Marker Analysis to Assess Valsartan's Efficacy in Mitigating Dasatinib-Induced Cardiac Toxicity in Sprague-Dawley Rats. [Abstract]2024 Dec 5:18:5641-5654. PMID: 39654603 -
Drug Des Devel Ther
Silibinin Augments the Antifibrotic Effect of Valsartan Through Inactivation of TGF-β1 Signaling in Kidney. [Abstract]2020 Feb 13;14:603-611. PMID: 32103902 -
Int J Mol Sci
2023 Feb 3;24(3):2960. PMID: 36769281 -
Front Pharmacol
Lcz696 Alleviates Myocardial Fibrosis After Myocardial Infarction Through the sFRP-1/Wnt/β-Catenin Signaling Pathway. [Abstract]2021 Sep 2;12:724147. PMID: 34539406 -
Eur J Pharmacol
Sacubitril/valsartan attenuates atrial electrical and structural remodelling in a rabbit model of atrial fibrillation. [Abstract]2020 Aug 15;881:173120. PMID: 32325147 -
Heliyon
The effect of novel antihypertensive drug valsartan on lysozyme aggregation: A combined in situ and in silico study. [Abstract]2023 Apr 10;9(4):e15270. PMID: 37123968 -
Kaohsiung J Med Sci
Sacubitril/Valsartan Ameliorates Inflammation and Oxidative Stress in Hypertensive Heart Disease by Upregulating CAMKK2 Protein and Modulating the AMPK/AKT/GSK-3β Axis. [Abstract]2025 Oct 17:e70127. PMID: 41104684 -
Ren Fail
LCZ696, an angiotensin receptor-neprilysin inhibitor, ameliorates epithelial-mesenchymal transition of peritoneal mesothelial cells and M2 macrophage polarization. [Abstract]2024 Dec;46(2):2392849. PMID: 39165231 -
Arch Biochem Biophys
Sacubitril/valsartan attenuates myocardial ischemia/reperfusion injury via inhibition of the GSK3β/NF-κB pathway in cardiomyocytes. [Abstract]2022 Nov 15:730:109415. PMID: 36179911 -
Mol Biol Rep
Cardiac drug potential: exploring individual and combined cardiac drugs to promote differentiation of adipose-derived stem cells into cardiomyocytes. [Abstract]2026 Feb 26;53(1):434. PMID: 41746444 -
J Cardiovasc Transl Res
Sacubitril/Valsartan Decreases Atrial Fibrillation Susceptibility by Inhibiting Angiotensin II-Induced Atrial Fibrosis Through p-Smad2/3, p-JNK, and p-p38 Signaling Pathways. [Abstract]2022 Feb;15(1):131-142. PMID: 34075552 -
Biomed Res Int
Effects of Sacubitril/Valsartan on the Expression of CaMKII/Cav1.2 in Atrial Fibrillation Stimulation Rabbit Model. [Abstract]2022 Jul 28:2022:5832543. PMID: 38550555 -
Physiol Res
(Pro)renin receptor contributes to hypoxia/reoxygenation-induced apoptosis and autophagy in myocardial cells via the beta-catenin signaling pathway. [Abstract]2020 Jul 16;69(3):427-438. PMID: 32469229 -
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Res Sq
Vactosertib, a novel TGF-β1 type I receptor kinase inhibitor, improves T-cell fitness: a single-arm, phase 1b trial in relapsed/refractory multiple myeloma. [Abstract]2023 Jul 17:rs.3.rs-3112163. PMID: 37503043
溶剤 & 溶解度
DMSO : 50 mg/mL (114.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.74 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (22.96 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Rats: Rats are randomly divided into two groups: (i) valsartan-treated group that is given intravenously 3 mg/kg/day valsartan in 0.5 mL normal saline via the vein daily for 1 week; (ii) hydralazine-treated group receiving 0.2 mg/kg/day hydralazine injection in saline; and (iii) control group that receives saline injection in the 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) is administered by oral (p.o.) route in a volume of 10 mL/kg body weight using the gavage technique. Potential alteration in blood pressure in response to chronic treatment with valsartan is assessed with a commercial blood pressure analysis systemdesigned. The mice are trained for at least 2 consecutive days to adapt to the apparatus before the study is initiated. To record the blood pressure, the mice are placed on a heated pad (35°C) and measured with a programmable tail-cuff sphygmomanometer in steady state. The average of 10 readings from each mouse is recorded[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (285 KB)
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- English - EN (419 KB)
- Français - FR (419 KB)
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- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Shan H, et al. Valsartan ameliorates ageing-induced aorta degeneration via angiotensin II type 1 receptor-mediated ERK activity. J Cell Mol Med. 2014 Jun;18(6):1071-80. [Content Brief]
[2]. Wang Y, et al. Valsartan blocked alcohol-induced, Toll-like receptor 2 signaling-mediated inflammation in human vascular endothelial cells. Alcohol Clin Exp Res. 2014 Oct;38(10):2529-40. [Content Brief]
[3]. Sui X, et al. Novel mechanism of cardiac protection by valsartan: synergetic roles of TGF-β1 and HIF-1α in Ang II-mediated fibrosis after myocardial infarction. J Cell Mol Med. 2015 Aug;19(8):1773-82. [Content Brief]
[4]. Jiang Y, et al. Cardioprotective effect of valsartan in mice with short-term high-salt diet by regulating cardiac aquaporin 1 and angiogenic factor expression. Cardiovasc Pathol. 2015 Jul-Aug;24(4):224-9. [Content Brief]
[5]. Ping G, et al. Valsartan reverses depressive/anxiety-like behavior and induces hippocampal neurogenesis and expression of BDNF protein in unpredictable chronic mild stress mice. Pharmacol Biochem Behav. 2014 Sep;124:5-12. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2961 mL | 11.4805 mL | 22.9611 mL | 57.4026 mL |
| 5 mM | 0.4592 mL | 2.2961 mL | 4.5922 mL | 11.4805 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2961 mL | 5.7403 mL | |
| 15 mM | 0.1531 mL | 0.7654 mL | 1.5307 mL | 3.8268 mL | |
| 20 mM | 0.1148 mL | 0.5740 mL | 1.1481 mL | 2.8701 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9184 mL | 2.2961 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9134 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4351 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1481 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3827 mL | 0.9567 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL | 0.5740 mL |
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