1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Valsartan

Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research.

For research use only. We do not sell to patients.

CAS No. : 137862-53-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Valsartan:

Top Publications Citing Use of Products

    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.

    Valsartan purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Jun:114:154747.

    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.

    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.

    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.

    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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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].

    IC50 & Target

    AT1 Receptor

     

    In Vitro

    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.

    In Vivo

    Valsartan (CGP 48933) significantly attenuates the expression of TGF-β/Smad, Hif-1α and fibrosis-related protein in rats after MI. Heart function, infarcted size, wall thickness as well as myocardial vascularization of ischaemic hearts are also significantly improved by valsartan compared with saline and hydralazine[3].
    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.

    Clinical Trial
    Molecular Weight

    435.52

    Formula

    C24H29N5O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)[C@@H](C(O)=O)N(C(CCCC)=O)CC1=CC=C(C2=CC=CC=C2C3=NNN=N3)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (22.96 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.97%

    References
    Animal Administration
    [4]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    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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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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