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Chemical Structure| 123524-52-7 Chemical Structure| 123524-52-7

Structure of Azelnidipine
CAS No.: 123524-52-7

Chemical Structure| 123524-52-7

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Azelnidipine is a dihydropyridine L-type calcium channel blocker and an antihypertensive.

Synonyms: CS 905; RS 9054; CCRIS 8650

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Product Details of Azelnidipine

CAS No. :123524-52-7
Formula : C33H34N4O6
M.W : 582.65
SMILES Code : 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; RS 9054; CCRIS 8650
MDL No. :MFCD00865803
InChI Key :ZKFQEACEUNWPMT-UHFFFAOYSA-N
Pubchem ID :65948

Safety of Azelnidipine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
LX-2 cells 100 nM 6 h Azelnidipine significantly reduced the increase in intracellular ROS levels induced by TGF-β1, Ang II, or H2O2 PMC3346246
LX-2 cells 100 nM 24 h Azelnidipine significantly reduced the up-regulation of COL1A1 mRNA expression induced by 5 ng·mL-1 TGF-β1 alone PMC3346246
guinea-pig portal vein myocytes 300 nM 7 min To investigate the inhibitory effects of Azelnidipine on voltage-dependent L-type Ca2+ channels, results showed persistent inhibition of IBa PMC2014663
SHEE 0, 1, 2.5, 5, 10, 15, 20 μM 24, 48, 72, 96 h To evaluate the effect of Azelnidipine on SHEE cell proliferation, results showed that Azelnidipine did not significantly inhibit SHEE cell proliferation. PMC9574346
KYSE450 0, 1, 2.5, 5, 10, 15, 20 μM 24, 48, 72, 96 h To evaluate the inhibitory effect of Azelnidipine on ESCC cell proliferation, results showed that Azelnidipine significantly inhibited ESCC cell proliferation in a concentration- and time-dependent manner. PMC9574346
KYSE150 0, 1, 2.5, 5, 10, 15, 20 μM 24, 48, 72, 96 h To evaluate the inhibitory effect of Azelnidipine on ESCC cell proliferation, results showed that Azelnidipine significantly inhibited ESCC cell proliferation in a concentration- and time-dependent manner. PMC9574346
CT26 cells 20 μM 24 h To test the effect of azelnidipine on the expression of CD47 and PVR in CT26 cells. Results showed that azelnidipine could inhibit the expression of PVR but not CD47. PMC8150775
BMDM cells 20 μM 4 h To test the effect of azelnidipine on macrophage phagocytosis of tumor cells. Results showed that azelnidipine significantly enhanced the phagocytosis of MC38, CT26, and B16-OVA tumor cells by BMDM cells. PMC8150775

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats STZ-induced diabetic model Oral gavage 5 mg/kg Once daily for 12 weeks To investigate the protective effect of Azelnidipine on hyperglycemia-induced cardiac damage. Results showed that AZL treatment significantly reduced levels of cardiac damage markers (e.g., Troponin-1, CK-MB, CK-NAC, uric acid, LDH, and alkaline phosphatase), improved inflammatory cytokine and lipid profiles, and decreased oxidative stress markers. PMC3004822
Wistar rats STZ-induced diabetic model Oral gavage 5 mg/kg Once daily for 12 weeks To evaluate the effect of Azelnidipine on diabetic cardiomyopathy. Results showed that Azelnidipine significantly improved cardiac contractile function, calcium handling protein expression, oxidative stress, and apoptosis. PMC3234183
C57BL/6 mice CCl4- or TAA-induced liver fibrosis model Oral 10 mg/kg 6 days a week for 6 weeks Azelnidipine significantly decreased inflammatory cell infiltration, pro-fibrotic gene expressions, HSC activation, lipid peroxidation, oxidative DNA damage and fibrosis in the livers of CCl4- or TAA-treated mice PMC3346246
SCID/CB17 mice Esophageal cancer patient-derived xenograft (PDX) model Oral gavage 2, 20 mg/kg Daily for 18 or 42 days To evaluate the inhibitory effect of Azelnidipine on esophageal cancer growth in vivo, results showed that Azelnidipine significantly inhibited tumor growth and reduced the levels of Ki67 and p-ERK1/2 T202/Y204. PMC9574346
Mice MC38 and CT26 tumor models Intraperitoneal injection 2 or 5 mg/kg Once daily for two weeks To test the inhibitory effect of azelnidipine on the growth of MC38 and CT26 tumors. Results showed that azelnidipine significantly inhibited tumor growth and enhanced the infiltration and function of CD8+ T cells. PMC8150775
Wistar rats Hypertension model Oral 9.7 mg/day 14 days Azelnidipine alleviated NA-induced blood pressure variability augmentation and preserved baroreceptor reflex sensitivity despite a smaller reduction in blood pressure PMC10994831

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00134160 Hypertension ... More >>Cardiovascular Diseases Less << Phase 4 Completed - Japan ... More >> Department of Cardiovascular Medicine Graduate School of Medical Science Kumamoto University 1-1-1 Honjyo, Kumamoto-City, Kumamoto, Japan, 860-8556 OSCAR-Study Data Center ShinjukuParkTower30FN, 3-7-1 Nishi-Shinjuku, Shinjuku-ku, Tokyo, Japan, 163-1030 Less <<
NCT01819441 Cerebral Small Vessel Diseases Phase 4 Unknown December 2016 China, Beijing ... More >> Peking University First Hospital Recruiting Beijing, Beijing, China, 100034 Contact: Yining Huang       ynhuang@sina.com Less <<
NCT00607035 Hypertension Phase 4 Completed - Japan ... More >> Jichi Medical University School of Medicine Tochigi, Japan Less <<
NCT01028534 Obstructive Sleep Apnea ... More >> Hypertension Less << Not Applicable Completed - Japan ... More >> Kirigaoka Tsuda Hospital Kitakyushu, Japan Kyoto University Hospital Kyoto, Japan Less <<
NCT00294567 Hypertension ... More >>Coronary Atherosclerosis Less << Phase 4 Completed - Japan ... More >> Department of Cardiology, Juntendo University School of Medicine Tokyo, Japan Less <<
NCT00454662 Hypertension ... More >>Cardiovascular Disease Diabetes Less << Phase 4 Completed - Japan ... More >> COLM-Study Data Center Kamiyacho MT Bld.14F, 4-3-20 Toranomon Minato-ku, Tokyo, Japan, 105-0001 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.58mL

1.72mL

0.86mL

17.16mL

3.43mL

1.72mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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