2. Membrane Transporter/Ion Channel Neuronal Signaling MAPK/ERK Pathway
  3. Calcium Channel MEK
  4. Azelnidipine

Azelnidipine  (Synonyms: CS 905)

Cat. No.: HY-B0023 Purity: 99.66%
COA Handling Instructions

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Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects .

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

Azelnidipine Chemical Structure

Azelnidipine Chemical Structure

CAS No. : 123524-52-7

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10 mM * 1 mL in DMSO
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10 mg USD 92 In-stock
50 mg USD 290 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Azelnidipine:

Azelnidipine Related Antibodies

Top Publications Citing Use of Products

View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

View All MEK Isoform Specific Products:

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MEK1 MEK2 MEK5 MEK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects [1] [2] [3].

IC50 & Target

L-type calcium channel

 

MEK1

 

MEK2

 

In Vitro

Azelnidipine (0-10 μM; 96 h) inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2 [2].

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

Azelnidipine Related Antibodies

Cell Proliferation Assay[2]

Cell Line: ESCC and SHEE cells
Concentration: 0, 1, 2.5, 5 and 10 μM
Incubation Time: 96 h
Result: Inhibited the proliferation of ESCC cells in a concentration- and time-dependent manner and did not significantly inhibit the proliferation of SHEE cells.

Western Blot Analysis[2]

Cell Line: ESCC cells
Concentration: 0, 1, 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Reduced MEK1/2 phosphorylation in a dose-dependent manner.
In Vivo

Azelnidipine (3 mg/kg/day; Oral gavage; 7 days) plays a protective role in rat models of cerebral ischemia-reperfusion [3].
Azelnidipine (0-3 mg/kg; Oral administration/Intravenous injection; 0-24 h) reduces blood pressure in hypertensive rat models. Oral efficacy is more than three times of Nicardipine (HY-12515). Intravenous injection is three times less effective than Nicardipine (HY-12515) [4].

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

Animal Model: BCCAO and reperfusion treated adult male Sprague-Dawley rats (200-300 g) [3]
Dosage: 3 mg/kg/day
Administration: Oral gavage (i.g.); 7 days
Result: Significantly increased total antioxidant capacity.
Reduced IL-6, TNF-α, NF-κB p65, and ICAM-1 levels.
Reversed the ischemic injury after cerebral ischemia/reperfusion and reduced cerebral infarct volume in rats.
Animal Model: Male spontaneously hypertensive rats aged 23 weeks old [4]
Dosage: 0.3, 1 and 3 mg/kg;
100 and 300 μg/kg
Administration: Oral administration (p.o.); single dose; 0-24 h;
Intravenous injection (i.v.); single dose; 0-2 h
Result: Reduced blood pressure in a dose-dependent manner, was more than 3 times as potent as Nicardipine (HY-12515) by p.o.
Gradually decreased blood pressure, was 3 times less potent than Nicardipine (HY-12515) by i.v.
Clinical Trial
Molecular Weight

582.65

Formula

C33H34N4O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(N)NC(C)=C(C(OC(C)C)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC3CN(C(C4=CC=CC=C4)C5=CC=CC=C5)C3
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 : ≥ 100 mg/mL (171.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7163 mL 8.5815 mL 17.1630 mL
5 mM 0.3433 mL 1.7163 mL 3.4326 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)

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 (4.29 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.
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).
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: 99.66%

COA (256 KB) LCMS (274 KB)

Handling Instructions (2659 KB)
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 1.7163 mL 8.5815 mL 17.1630 mL 42.9074 mL
5 mM 0.3433 mL 1.7163 mL 3.4326 mL 8.5815 mL
10 mM 0.1716 mL 0.8581 mL 1.7163 mL 4.2907 mL
15 mM 0.1144 mL 0.5721 mL 1.1442 mL 2.8605 mL
20 mM 0.0858 mL 0.4291 mL 0.8581 mL 2.1454 mL
25 mM 0.0687 mL 0.3433 mL 0.6865 mL 1.7163 mL
30 mM 0.0572 mL 0.2860 mL 0.5721 mL 1.4302 mL
40 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0727 mL
50 mM 0.0343 mL 0.1716 mL 0.3433 mL 0.8581 mL
60 mM 0.0286 mL 0.1430 mL 0.2860 mL 0.7151 mL
80 mM 0.0215 mL 0.1073 mL 0.2145 mL 0.5363 mL
100 mM 0.0172 mL 0.0858 mL 0.1716 mL 0.4291 mL
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Azelnidipine 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:

Azelnidipine123524-52-7CS 905CS905CS-905Calcium ChannelMEKCa2+ channelsCa channelsMitogen-activated protein kinase kinaseMAPKKMAP2KCalcium channel blockerAntihypertensive agentESCC cellsCerebral ischemia-reperfusion injury modelInhibitorinhibitorinhibit

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