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Chemical Structure| 132203-70-4 Chemical Structure| 132203-70-4

Structure of Cilnidipine
CAS No.: 132203-70-4

Chemical Structure| 132203-70-4

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Cilnidipine is a dual L- and N-type calcium channel blocker with antihypertensive, sympatholytic and neuroprotective activity.

Synonyms: FRC-8653

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Product Details of Cilnidipine

CAS No. :132203-70-4
Formula : C27H28N2O7
M.W : 492.52
SMILES Code : O=C(C1=C(C)NC(C)=C(C(OCCOC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC/C=C/C3=CC=CC=C3
Synonyms :
FRC-8653
MDL No. :MFCD00865853
InChI Key :KJEBULYHNRNJTE-DHZHZOJOSA-N
Pubchem ID :5282138

Safety of Cilnidipine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 1 µM 24 hours Evaluate the effect of SR9009 on BMAL1 mRNA expression PMC11122359

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Ob/ob mice Obese model 5 mg/kg/day, then increased to 20 mg/kg/day intraperitoneal 6 weeks continuously Improved liver injury and lipid droplet accumulation, increased mitochondria-lipid droplet contact PMC11122359

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00541853 Kidney, Polycystic, Autosomal ... More >>Dominant Less << Phase 4 Unknown November 2012 Japan ... More >> Kyorin University School of Medicine Not yet recruiting Mitaka, Tokyo, Japan, 181-8611 Contact: Eiji Higashihara, M.D.    81+422475511 ext 5813    ehigashi@kyorin-u.ac.jp    Contact: Kikuo Nutahara, M.D.    81-422475511 ext 5815    kinuta@kyorin-u.ac.jp    Department of Urology, National Hospital Organaization Chiba-East Hospital Not yet recruiting Chiba, Chiba, Japan, 260-8712 Contact: Koichi Kamura, MD    81+432615171 ext 7607    kamura@cehpnet.com    Toranomon Hospital Kajigaya, Kidney center Not yet recruiting Kanagawa, Japan, 213-8587 Contact: Yoshifumi Ubara, MD    81+448775111 ext 6064    ubara@toranomon.gr.jp    Toranomon Hospital, Kidney center Not yet recruiting Tokyo, Japan, 105-8470 Contact: Kenmei Tkaichi, MD    81+335881111 ext 7065    takaichi@toranomon.gr.jp    Division of Kidney and Hypertension, Department of Internal Medicine, Jikei University School of Medicine Not yet recruiting Tokyo, Japan, 105-8471 Contact: Tatsuo Hosoya, MD    81+334331111 ext 3220    t-hosoya@jikei.ac.jp    Contact: Kazushige Hanaoka, MD    81+334331111 ext 3221    khanaoka@jikei.ac.jp    Department of Urology, Teikyo University, School of Medicine Not yet recruiting Tokyo, Japan, 173-8605 Contact: Shigeo Horie, MD    81+339641211    shorie@med.teikyo-u.ac.jp    Contact: Satoru Muto, MD    81+33964-1211    muto@med.teikyo-u.ac.jp Less <<
NCT02145104 Hypertension Phase 3 Completed - Korea, Republic of ... More >> Seoul National University Bundang Hospital Seongnam-si, Kyung-gi, Korea, Republic of Less <<
NCT00890279 Kidney, Polycystic, Autosomal ... More >>Dominant Less << Phase 2 Unknown November 2012 Japan ... More >> Department of Medicine II, Hokkaido Univserity School of Medicine Recruiting Sapporo, Hokkaido, Japan, 0608638 Contact: Toshio Mochizuki, MD    +81117065915    mtoshi@med.hokudai.ac.jp    Principal Investigator: Toshio Mochizuki, MD          Toranomon Hospital Kajigaya, Kidney center Not yet recruiting Kawasaki, Kanagawa, Japan, 2138587 Contact: Yoshihumi Ubara, MD    +81448775111 ext 6064    ubara@toranomon.gr.jp    Principal Investigator: Yoshihumi Ubara, MD          Department of Medicine II, Nippon Medical School Not yet recruiting Bunkyo-ku, Tokyo, Japan, 1138602 Contact: Yasuhiko Iino, MD    +81338222131    iinoyasuhiko@nms.ac.jp    Principal Investigator: Yasuhiko Iino, MD          Department of Urology, Teikyo University School of Medicine Recruiting Itabashi-ku, Tokyo, Japan, 1738605 Contact: Shigeo Horie, MD    +81339642497    shorie@med.teikyo-u.ac.jp    Contact: Satoru Muto, MD    +81339642497    muto@med.teikyo-u.ac.jp    Principal Investigator: Shigeo Horie, MD          Toranomon Hospital, Kidney center Not yet recruiting Minato-ku, Tokyo, Japan, 1058470 Contact: Kenmei Takaichi, MD    +81335881111 ext 7065    takaichi@toranomon.gr.jp    Principal Investigator: Kenmei Takaichi, MD          Division of Kidney and Hypertension, Department of Internal Medicine, Jikei University School of Medicine Active, not recruiting Minato-ku, Tokyo, Japan, 1058471 Department of Urology, Kyorin University School of Medicine Not yet recruiting Mitaka, Tokyo, Japan, 1818611 Contact: Eiji HIgashihara, MD    81422475511    ehigashi@kyorin-u.ac.jp    Contact: Kikuo Nutahara, MD    81422475511    kinuta@kyorin-u.ac.jp    Principal Investigator: Eiji Higashihara, MD          Sub-Investigator: Kikuo Nutahara, MD          Department of Urology, National Hospital Organaization Chiba-East Hospital Not yet recruiting Chiba, Japan, 2608712 Contact: Koichi Kamura, MD    +81432615171 ext 7607    kamura@cehpnet.com    Principal Investigator: Koichi Kamura, MD          Division of Clinical Nephrology and Rheumatology, Niigata University Graduate School of Medical and Dental Sciences Not yet recruiting Niigata, Japan, 9518510 Contact: Ichiei Narita, MD    +813252272193    naritai@med.niigata-u.ac.jp    Principal Investigator: Ichiei Narita, MD Less <<
NCT02343250 Hypertension Phase 1 Completed - -
NCT02088008 Healthy Volunteers Phase 1 Unknown - Korea, Republic of ... More >> Seoul National University Hospital Not yet recruiting Seoul, Korea, Republic of Contact: Kyungsang Yu          Principal Investigator: Kyungsang Yu Less <<
NCT01838967 Healthy Phase 1 Completed - Korea, Republic of ... More >> Seoul National University Hospital Jongno-gu, Seoul, Korea, Republic of, 110-744 Less <<
NCT00325637 Hypertension ... More >>Stroke Less << Phase 3 Completed - Korea, Republic of ... More >> Seoul National University Budang Hospital Seongnam-si, Gyeonggi-do, Korea, Republic of Less <<
NCT00325936 Hypertension|Metabolic Syndrom... More >>e X Less << PHASE4 COMPLETED 2025-06-07 Cheil general hospital, Seoul,... More >> 100-380, Korea, Republic of Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.15mL

2.03mL

1.02mL

20.30mL

4.06mL

2.03mL

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
Protocol 2

References

[1]Takahara A, Fujita S, et al. Neuronal Ca2+ channel blocking action of an antihypertensive drug, cilnidipine, in IMR-32 human neuroblastoma cells. Hypertens Res. 2003 Sep;26(9):743-7.

[2]Shiomi T, Tsutsui H, et al. Pioglitazone, a peroxisome proliferator-activated receptor-gamma agonist, attenuates left ventricular remodeling and failure after experimental myocardial infarction. Circulation. 2002 Dec 10;106(24):3126-32.

[3]Masuda T, Ogura MN, Moriya T, et al. Beneficial effects of L- and N-type calcium channel blocker on glucose and lipid metabolism and renal function in patients with hypertension and type II diabetes mellitus. Cardiovasc Ther. 2011;29(1):46‐53

[4]Murai Y, Uneyama H, Ishibashi H, Takahama K, Akaike N. Preferential inhibition of L- and N-type calcium channels in the rat hippocampal neurons by cilnidipine. Brain Res. 2000;854(1-2):6‐10

[5]Takahara A, Konda T, Enomoto A, Kondo N. Neuroprotective effects of a dual L/N-type Ca(2+) channel blocker cilnidipine in the rat focal brain ischemia model. Biol Pharm Bull. 2004;27(9):1388‐1391

[6]Morimoto S, Yano Y, Maki K, Iwasaka T. Renal and vascular protective effects of cilnidipine in patients with essential hypertension. J Hypertens. 2007;25(10):2178‐2183

[7]Tajiri K, Guichard JB, Qi X, et al. An N-/L-type calcium channel blocker, cilnidipine, suppresses autonomic, electrical, and structural remodelling associated with atrial fibrillation. Cardiovasc Res. 2019;115(14):1975‐1985

[8]Shete MM. Cilnidipine: Next Generation Calcium Channel Blocker. J Assoc Physicians India. 2016;64(4):95‐99

 

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