1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Azilsartan (medoxomil monopotassium)

Azilsartan (medoxomil monopotassium)  (Synonyms: Azilsartan kamedoxomil; TAK 491 monopotassium)

Cat. No.: HY-17458 Purity: 98.00%
Handling Instructions Technical Support

Azilsartan medoxomil (TAK 491) monopotassium, a prodrug form of Azilsartan (HY-14914), is an orally active angiotensin II receptor type 1 antagonist. Azilsartan medoxomil monopotassium can be used for the study of essential hypertension.

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Azilsartan (medoxomil monopotassium)

Azilsartan (medoxomil monopotassium) 화학구조

CAS No. : 863031-24-7

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Azilsartan (medoxomil monopotassium):

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Azilsartan (medoxomil monopotassium)

View All Angiotensin Receptor Isoform Specific Products:

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Azilsartan medoxomil (TAK 491) monopotassium, a prodrug form of Azilsartan (HY-14914), is an orally active angiotensin II receptor type 1 antagonist. Azilsartan medoxomil monopotassium can be used for the study of essential hypertension[1][2][3][4].

IC50 & Target

AT1 Receptor

 

In Vivo

Azilsartan medoxomil (0.03-1 mg/kg, p.o.) monopotassium inhibits the angiotensin II-induced pressor response in normotensive rats[2].
Azilsartan medoxomil (0.1-10 mg/kg in peanut butter, once daily) monopotassium inhibits vascular wall expression of plasminogen activator inhibitor type-I (PAI-1) protein, and potentially facilitates the stabilization of atherosclerotic plaques in ApoE knockout mice on a high fat diet rendered overexpressors of PAI-1 in VSMCs[5].
Azilsartan medoxomil (0.03-10 mg/kg, oral gavage, once a day) monopotassium reduces myocardial infarct size in rats[6].

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

Animal Model: Rats[6]
Dosage: 0.03-10 mg/kg
Administration: oral gavage, once a day for 4 days
Result: Reduced myocardial infarct size.
Increased calcium-dependent nitric oxide synthase activity.
Increased Akt, ERK 1/2 and eNOS phosphorylation and inhibited BAX activation.
분자량

606.62

화학식

C30H23KN4O8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C5=NC(O[N-]5)=O)C=C3)=CC=C1)OCC6=C(C)OC(O6)=O.[K+]

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도
In Vitro: 

DMSO : 175 mg/mL (288.48 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 1.6485 mL 8.2424 mL 16.4848 mL
5 mM 0.3297 mL 1.6485 mL 3.2970 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

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: ≥ 3 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 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 (30.0 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 (sealed storage, away from moisture)

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.
순도&문서
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 (sealed storage, away from moisture). 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 1.6485 mL 8.2424 mL 16.4848 mL 41.2120 mL
5 mM 0.3297 mL 1.6485 mL 3.2970 mL 8.2424 mL
10 mM 0.1648 mL 0.8242 mL 1.6485 mL 4.1212 mL
15 mM 0.1099 mL 0.5495 mL 1.0990 mL 2.7475 mL
20 mM 0.0824 mL 0.4121 mL 0.8242 mL 2.0606 mL
25 mM 0.0659 mL 0.3297 mL 0.6594 mL 1.6485 mL
30 mM 0.0549 mL 0.2747 mL 0.5495 mL 1.3737 mL
40 mM 0.0412 mL 0.2061 mL 0.4121 mL 1.0303 mL
50 mM 0.0330 mL 0.1648 mL 0.3297 mL 0.8242 mL
60 mM 0.0275 mL 0.1374 mL 0.2747 mL 0.6869 mL
80 mM 0.0206 mL 0.1030 mL 0.2061 mL 0.5151 mL
100 mM 0.0165 mL 0.0824 mL 0.1648 mL 0.4121 mL
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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.

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상품명:
Azilsartan (medoxomil monopotassium)
Cat. No.:
HY-17458
수량:
MCE Japan Authorized Agent: