2. GPCR/G Protein
  3. Angiotensin Receptor
  4. Allisartan isoproxil

Allisartan isoproxil (ALS-3) is an orally potent, selective, non-peptide inhibitor of Angiotensin II Type 1. Allisartan isoproxil is also an antihypertensive agent. Allisartan isoproxil may inhibit angiotensin-aldosterone system and oxidative stress. Allisartan isoproxil lowers blood pressure and protects the organs, preventing cerebrovascular damage. Allisartan isoproxil (80-320 mg/kg/d) has shown toxicity in rat models by targeting liver organs.

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Allisartan isoproxil Chemical Structure

Allisartan isoproxil Chemical Structure

CAS No. : 947331-05-7

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Description

Allisartan isoproxil (ALS-3) is an orally potent, selective, non-peptide inhibitor of Angiotensin II Type 1. Allisartan isoproxil is also an antihypertensive agent. Allisartan isoproxil may inhibit angiotensin-aldosterone system and oxidative stress. Allisartan isoproxil lowers blood pressure and protects the organs, preventing cerebrovascular damage. Allisartan isoproxil (80-320 mg/kg/d) has shown toxicity in rat models by targeting liver organs[1][2].

IC50 & Target[1]

Angiotensin II Type 1

 

In Vivo

The metabolic pathway of Allisartan isoproxil is relatively simple, and Allisartan isoproxil is completely and directly converted to EXP-3174 by esterase during gastrointestinal absorption[1].
Allisartan isoproxil (20, 80 and 320 mg/kg/day; po; for 26 weeks) decreases body weight at 80-320 mg/kg/day dose, in Sprague-Dawley rats[1].
Allisartan isoproxil (30 mg/kg/day; po in diet; for 55 weeks) significantly decreases stroke-related death and prolongs lifespan in stroke-prone renovascular hypertensive rats (RHR-SP)[2].

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

Animal Model: Femal and male Sprague-Dawley rats[1]
Dosage: 20, 80 and 320 mg/kg
Administration:
Result: Decreased body-weight gain at 320 mg/kg/day in both sexes as well as at the 80-mg/kg/day dose in females.
Decreased erythrocyte parameters in males, and decreased heart weight and exacerbation of chronic progressive nephropathy (CPN) severity in males at 80 and 320 mg/kg/day.
Clinical Trial
Molecular Weight

553.01

Formula

C27H29ClN6O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)OCOC(OC(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (180.83 mM; ultrasonic and warming and heat to 60°C; 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 1.8083 mL 9.0414 mL 18.0829 mL
5 mM 0.3617 mL 1.8083 mL 3.6166 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (4.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (4.52 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.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
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 (protect from light). 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 1.8083 mL 9.0414 mL 18.0829 mL 45.2071 mL
5 mM 0.3617 mL 1.8083 mL 3.6166 mL 9.0414 mL
10 mM 0.1808 mL 0.9041 mL 1.8083 mL 4.5207 mL
15 mM 0.1206 mL 0.6028 mL 1.2055 mL 3.0138 mL
20 mM 0.0904 mL 0.4521 mL 0.9041 mL 2.2604 mL
25 mM 0.0723 mL 0.3617 mL 0.7233 mL 1.8083 mL
30 mM 0.0603 mL 0.3014 mL 0.6028 mL 1.5069 mL
40 mM 0.0452 mL 0.2260 mL 0.4521 mL 1.1302 mL
50 mM 0.0362 mL 0.1808 mL 0.3617 mL 0.9041 mL
60 mM 0.0301 mL 0.1507 mL 0.3014 mL 0.7535 mL
80 mM 0.0226 mL 0.1130 mL 0.2260 mL 0.5651 mL
100 mM 0.0181 mL 0.0904 mL 0.1808 mL 0.4521 mL
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Allisartan isoproxil Related Classifications

Help & FAQs
  • 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.

Keywords:

Allisartan isoproxil947331-05-7Angiotensin Receptorangiotensin receptor blockerblood pressurehypertensionorgan damagestrokeInhibitorinhibitorinhibit

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