| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| 10g |
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Purity: =99.11%
Valsartan (formerly CGP-48933; CGP48933; Diovan, Prova, Tareg, Miten, Nisis, Vals, Walsarta), an approved antihypertensive drug, is a potent and selective angiotensin II receptor antagonist that is used for the treatment of high blood pressure and congestive heart failure. Valsartan is selective for the type I (AT1) angiotensin receptor. Valsartan dose-dependently inhibits the vasoconstriction induced by angiotensin II and lowers blood pressure in renin-dependent models of hypertension.
| Targets |
Angiotensin II receptor
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|---|---|
| ln Vitro |
By inhibiting the action of angiotensin, valsartan (CGP 48933), a synthetic non-peptide angiotensin II type 1 receptor antagonist, dilates blood vessels and lowers blood pressure. Ageing aortic endothelial cells exhibit a substantial reduction in AT1R expression when treated with valsartan[1]. Proinflammatory cytokines and TLR2 signaling are inhibited when valsartan is pretreated. Following alcohol consumption, the expression of AGTR1 is up-regulated, and valsartan pretreatment blocks this expression[2].
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| ln Vivo |
In rats with MI, valsartan (CGP 48933) dramatically reduces the expression of TGF-β/Smad, Hif-1α, and fibrosis-related protein. Comparing valsartan to saline and hydralazine, there is a considerable improvement in cardiac function, infarcted size, wall thickness, and myocardial vascularization of ischemic hearts[3]. A high-salt diet can cause hypertension, heart damage such fibrosis and inflammatory cell infiltration, suppression of aquaporin 1 and angiogenic factors, and other consequences that valsartan can partially reverse[4]. Valsartan is a potent antidepressant and anti-anxiety medication that can increase BDNF expression and hippocampus neurogenesis. Long-term valsartan administration (5–40 mg/kg/d, po) decreases immobility time in TST and FST, lengthens the time in the center of the field in OFT and the latency to eat in NSF, and enhances the preference for sucrose in SPT[5].
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| Enzyme Assay |
The aorta tissue or cell samples were homogenized in lysis buffer A (20 mM Tris-HCl, pH8.0, 150 mM NaCl, 1% Triton X-100, 2 mM EDTA, 1 mM phenylmethylsulfonyl fluoride, 20 μg/ml aprotinin, 10 μg/ml leupeptin, 20 mM ß-glycerophate, and 2 mM NaF) for 30 min. The homogenates were centrifugated and protein concentration was determined with BCA protein assay reagent kit (Piece Biotech Inc., Rockford, IL, USA). An equal amount of protein (20 μg/lane for most proteins, while 100 μg/lane for p-p38 and p-JNK detection) from each sample extract was loaded in a 12.5% SDS-PAGE gel for Electrophoresis, and electroblotted onto PDVF membrane. Membrane was blocked with 5% non-fat dried milk (in TBST) for 2 hrs at room temperature and then incubated with primary antibody overnight at 4°C Then, membrane was washed with TBST (10 min. ×3) and incubated with horseradish peroxidase-conjugated secondary antibodies for 1 hr at room temperature (All the antibodies were purchased from Cell Signaling Technology, Boston, MA, USA). After washing with TBST (10 min. ×3), the immunoblots were developed using an ECL Western blotting detection system (Amersham Pharmacia Biotech, Piscataway, NJ, USA) and recorded by exposure of the immunoblots to an X-ray film [1].
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| Cell Assay |
The aorta were cut into small pieces and fixed in 2.5% glutaraldehyde in 0.2 M cacodylate buffer (pH 7.4) at 4°C for 2 hrs, then washed in PBS. The materials were incubated in a 2% OsO4 solution, dehydrated in a series of increasing ethanol concentrations and propylene oxide, and finally were immersed in Spurr resin. Ultrathin sections (50 nm) were cut on a Leica ultracut UCT ultramicrotome (Leica Microsystems Inc, LKB-II, Wetzlar, Germany), mounted on copper grids, and examined under a JEM 1200EX transmission electron microscope [1].
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| Animal Protocol |
Twenty young (or adult, 3-month-old) and 40 aged (18-month-old) male Wistar rats were purchased from the Department of Laboratory Animals, China Medical University. Animals were maintained at controlled temperature of 21°C and in a 12-hour day/night cycle. All the experimental procedures were approved by the Institutional Animal Care and Use Committee of China Medical University.
Young or adult animals were used as control group. Aged animals were randomly divided into two groups: the ageing group and Valsartan group (n = 20 in each group). The control and the ageing animals had free access to water and standard rat chow. The valsartan group animals continually took valsartan (Novartis Pharma Stein AG; 30 mg/kg/day) in their drinking water for 6 months. The concentration of valsartan dissolved in the drinking water was determined based on the previously established rats drinking patterns [1].
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| References |
[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.
[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. [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. [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. [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 |
| Molecular Formula |
C24H29N5O3
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|---|---|---|
| Molecular Weight |
435.52
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| Exact Mass |
435.227
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| Elemental Analysis |
C, 66.19; H, 6.71; N, 16.08; O, 11.02
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| CAS # |
137862-53-4
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| Related CAS # |
Sacubitril/Valsartan;936623-90-4;Valsartan-d9;1089736-73-1;Valsartan-d3;1331908-02-1;Valsartan-d8;1089736-72-0;(Rac)-Valsartan-d9; 137862-53-4; 149690-05-1 (sodium)
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| Appearance |
White to off-white solid
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| LogP |
4.75
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| tPSA |
112.070
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| SMILES |
O([H])C([C@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])N(C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)C([H])([H])C1C([H])=C([H])C(C2=C([H])C([H])=C([H])C([H])=C2C2N=NN([H])N=2)=C([H])C=1[H])=O
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| InChi Key |
ACWBQPMHZXGDFX-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1
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| Chemical Name |
(S)-3-methyl-2-(N-{[2-(2H-1,2,3,4-tetrazol-5-yl)biphenyl-4-yl]methyl}pentanamido)butanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (22.96 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2961 mL | 11.4805 mL | 22.9611 mL | |
| 5 mM | 0.4592 mL | 2.2961 mL | 4.5922 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2961 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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