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  2. Drug Derivative Angiotensin Receptor
  3. Valsartan methyl ester

Valsartan methyl ester  (Synonyms: CGP 48933 methyl ester)

Cat. No.: HY-W414915 Purity: 99.39%
Handling Instructions Technical Support

Valsartan (CGP 48933) methyl ester is the methyl ester derivative of Valsartan (HY-18204). Valsartan is a selective angiotensin II type 1 (AT1) receptor blocker (ARB) with potent antihypertensive and cardioprotective effects. Valsartan competitively binds to AT1 receptors, inhibiting the binding of angiotensin II to AT1 receptors, thereby blocking angiotensin II-mediated vasoconstriction, sodium retention, and myocardial hypertrophy signaling pathways. Valsartan reduces systolic blood pressure in L-NAME-induced hypertensive rats. Valsartan can be used for the study and treatment of arterial hypertension, hypertensive heart disease, and heart failure.

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Valsartan methyl ester

Valsartan methyl ester Chemical Structure

CAS No. : 137863-17-3

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Based on 1 publication(s) in Google Scholar

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Description

Valsartan (CGP 48933) methyl ester is the methyl ester derivative of Valsartan (HY-18204). Valsartan is a selective angiotensin II type 1 (AT1) receptor blocker (ARB) with potent antihypertensive and cardioprotective effects. Valsartan competitively binds to AT1 receptors, inhibiting the binding of angiotensin II to AT1 receptors, thereby blocking angiotensin II-mediated vasoconstriction, sodium retention, and myocardial hypertrophy signaling pathways. Valsartan reduces systolic blood pressure in L-NAME-induced hypertensive rats. Valsartan can be used for the study and treatment of arterial hypertension, hypertensive heart disease, and heart failure[1].

In Vivo

Valsartan (68 mg/kg, p.o., daily, dissolved in drinking water, 4 weeks) methyl ester significantly reduces systolic blood pressure in L-NAME-induced hypertensive adult male Wistar rats[1].

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

Animal Model: Adult (12-week-old) male Wistar rats were administered Nω-nitro-L-arginine methyl ester (L-NAME) at a dose of 40 mg/kg/day dissolved in drinking water for 4 weeks to induce hypertension and hypertensive heart disease[1]
Dosage: 68 mg/kg
Administration: p.o., daily, dissolved in drinking water, 4 weeks
Result: Achieved systolic blood pressure (SBP) reduction.
Showed no significant changes in body weight.
Reduced left ventricular weight (LVW).
Appeared increases in left ventricular ejection fraction (LVEF) and left ventricular fractional shortening (LVFS).
Reduced hydroxyproline concentration in insoluble collagen and total collagen.
Reduced the volume of type I collagen and type III collagen.
Reduced serum prolactin level and serum prolactin receptor level.
Showed decreases in E/A ratio, deceleration time (DecT), and isovolumic relaxation time.
Molecular Weight

449.55

Formula

C25H31N5O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC([C@H](C(C)C)N(C(CCCC)=O)CC1=CC=C(C=C1)C2=C(C3=NN=NN3)C=CC=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 175 mg/mL (389.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2244 mL 11.1222 mL 22.2445 mL
5 mM 0.4449 mL 2.2244 mL 4.4489 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • 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

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Volume (start)

V1

=
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C2

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V2

In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2244 mL 11.1222 mL 22.2445 mL 55.6112 mL
5 mM 0.4449 mL 2.2244 mL 4.4489 mL 11.1222 mL
10 mM 0.2224 mL 1.1122 mL 2.2244 mL 5.5611 mL
15 mM 0.1483 mL 0.7415 mL 1.4830 mL 3.7074 mL
20 mM 0.1112 mL 0.5561 mL 1.1122 mL 2.7806 mL
25 mM 0.0890 mL 0.4449 mL 0.8898 mL 2.2244 mL
30 mM 0.0741 mL 0.3707 mL 0.7415 mL 1.8537 mL
40 mM 0.0556 mL 0.2781 mL 0.5561 mL 1.3903 mL
50 mM 0.0445 mL 0.2224 mL 0.4449 mL 1.1122 mL
60 mM 0.0371 mL 0.1854 mL 0.3707 mL 0.9269 mL
80 mM 0.0278 mL 0.1390 mL 0.2781 mL 0.6951 mL
100 mM 0.0222 mL 0.1112 mL 0.2224 mL 0.5561 mL
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  • Do most proteins show cross-species activity?

    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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Valsartan methyl ester
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HY-W414915
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