Art. -Nr.: HY-B0023

Azelnidipine

(Synonyms: CS 905)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

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 .

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Reinheit: 99.79%
CAS. Nr.: 123524-52-7
Formel: C₃₃H₃₄N₄O₆
Molecular Weight:582.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Azelnidipine Chemical Structure

CAS. Nr.: 123524-52-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

L-type calcium channel

MEK1

MEK2

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Alle MEK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LLC-MK2	IC₅₀	2.9 μM Compound: Azelnidipine	Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay	[PMID: 20934347]
LLC-MK2	IC₅₀	33.48 μM Compound: Azelnidipine	Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay	[PMID: 20934347]

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 123524-52-7
Appearance Solid
Molecular Weight 582.65
Formel C₃₃H₃₄N₄O₆
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
Synonyms

CS 905
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Adv Mater

Efficient Delivery of Lomitapide using Hybrid Membrane-Coated Tetrahedral DNA Nanostructures for Glioblastoma Therapy. [Abstract]

2024 Jun;36(24):e2311760. PMID: 38569065
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
Viruses

Azelnidipine Exhibits In Vitro and In Vivo Antiviral Effects against Flavivirus Infections by Targeting the Viral RdRp. [Abstract]

2022 Jun 5;14(6):1228. PMID: 35746699

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7163 mL

8.5815 mL

17.1630 mL

5 mM

0.3433 mL

1.7163 mL

3.4326 mL

10 mM

0.1716 mL

0.8581 mL

1.7163 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Portuguese - PT (476 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ram CVS. Therapeutic Usefulness of a Novel Calcium Channel Blocker Azelnidipine in the Treatment of Hypertension: A Narrative Review. Cardiol Ther. 2022 Dec;11(4):473-489. [Content Brief]

[2]. Zhao L, et al. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation in vivo and in vitro by targeting MEK1/2. Mol Ther Oncolytics. 2022 Sep 26;27:61-72. [Content Brief]

[3]. Fakharaldeen Z, et al. Potential protective effects of Azelnidipine against cerebral ischemia-reperfusion injury in male rats. J Med Life. 2022 Nov;15(11):1384-1391. [Content Brief]

[4]. Oizumi K, et al. Antihypertensive effects of CS-905, a novel dihydropyridine Ca ⁺⁺ channel blocker. Jpn J Pharmacol. 1989 Sep;51(1):57-64. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Azelnidipine

3 Cited Publications

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Azelnidipine

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Publications Citing Use of MedChemExpress (MCE) Azelnidipine

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Azelnidipine Related Classifications

Art. -Nr.: HY-B0023