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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 100427-26-7 Chemical Structure| 100427-26-7

Structure of Lercanidipine
CAS No.: 100427-26-7

Chemical Structure| 100427-26-7

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Lercanidipine is a third-generation, lipophilic, blood-brain barrier-penetrant, orally active dihydropyridine calcium channel blocker with a pIC50 of 7.74 (converted from micromolar concentration). Lercanidipine has prolonged antihypertensive effects and renal and neuroprotective properties, as well as antioxidant, anti-inflammatory, and anti-apoptotic characteristics. Lercanidipine is used in cardiovascular and neurological research.

4.5 *For Research Use Only !

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Product Details of Lercanidipine

CAS No. :100427-26-7
Formula : C36H41N3O6
M.W : 611.73
SMILES Code : O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC(C)(C)CN(CCC(C3=CC=CC=C3)C4=CC=CC=C4)C
MDL No. :MFCD00867978

Safety of Lercanidipine

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P264-P270-P301+P310+P330-P405-P501
Class:6.1
UN#:2811
Packing Group:

Related Pathways of Lercanidipine

MAPK
pyroptosis
TLR

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
Vero cells 10 μM 1 h Screening for LUJV entry inhibitors Front Microbiol. 2021 Dec 2;12:793519.
Chang (normal liver cells) 10 μM 24 h Lercanidipine did not significantly increase the cytotoxicity of Bortezomib in normal cells Int J Mol Sci. 2019 Dec 4;20(24):6112.
MCF-10A (normal breast cells) 10 μM 24 h Lercanidipine did not significantly increase the cytotoxicity of Bortezomib in normal cells Int J Mol Sci. 2019 Dec 4;20(24):6112.
RPMI-8226 (multiple myeloma cells) 10 μM 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
BxPC-3 (pancreatic cancer cells) 10 μM 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
NCI-H460 (lung cancer cells) 10 μM 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
SNU-668 (stomach cancer cells) 10 μM 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
SNU-475 (liver cancer cells) 10 μM 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
MDA-MB 435S (breast cancer cells) 10 μM 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
Primary lung cancer cells 10 μM 24 h Inhibited the expression of PD-L1 Front Pharmacol. 2021 Jan 13;11:539261.
NCI-H460 cells 10 μM 24 h Inhibited the transcriptional levels of PD-L1 Front Pharmacol. 2021 Jan 13;11:539261.
NCI-H1299 cells 10 μM 24 h Inhibited the transcriptional levels of PD-L1 Front Pharmacol. 2021 Jan 13;11:539261.
A172GSC cells 7 μM Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
U251GSC cells 7 μM Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
GBM1 cells 7 μM Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
GSC11 cells 7 μM Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
OC-1 cells 0.3 to 2.5 µM 24 h To evaluate the antioxidative effect of Lercanidipine on OC-1 cell viability, results showed that 0.3 to 2.5 µM Lercanidipine significantly enhanced cellular viability Antioxidants (Basel). 2024 Mar 7;13(3):327.
CHO cells (expressing Ca v1.2b subunit) 10^-7 M 600 s To study the inhibitory effect of (S)-lercanidipine on vascular Ca v1.2b subunit, showing IC50=1.8×10^-8 M, Hill coefficient nH=0.8, indicating higher selectivity for the vascular isoform. Br J Pharmacol. 2004 May;142(2):275-84.
CHO cells (expressing Ca v1.2a subunit) 10^-7 M 600 s To study the inhibitory effect of (S)-lercanidipine on cardiac Ca v1.2a subunit, showing IC50=3.3×10^-8 M, Hill coefficient nH=2.3, indicating overlap between agonistic and antagonistic effects. Br J Pharmacol. 2004 May;142(2):275-84.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft tumor models Tail vein injection 5 mg/kg Twice every week for four weeks Suppressed tumor growth, reduced GLT8D1 and CD133 expression, increased apoptosis markers Cell Death Differ. 2022 Sep;29(9):1834-1849.
White New Zealand rabbits Atherosclerotic lesions induced by cholesterol feeding Subcutaneous injection 0.3, 1, and 3 mg/kg Once a week for 10 weeks Significantly reduced intimal hyperplasia and aortic fatty streak area in a dose-dependent manner Br J Pharmacol. 1998 Dec;125(7):1471-6
C57BL/6J mice Noise-induced hearing loss model Intraperitoneal injection 6 mg/kg 1 hour before noise exposure and once daily on days 1, 2, and 3 post-exposure To investigate the protective effect of Lercanidipine against noise-induced hearing loss, results showed that Lercanidipine significantly attenuated the elevation of hearing thresholds and preserved OHC survival in the basal turn Antioxidants (Basel). 2024 Mar 7;13(3):327.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00424801 Microvascular Angina ... More >> Hypertension Less << Not Applicable Terminated(Due to recent findi... More >>ngs relating MRI contrast to nephrogenic systemic fibrosis) Less << December 2008 Denmark ... More >> Aarhus Hospital Aarhus, Denmark, 8000 Less <<
NCT00741585 Essential Hypertension ... More >> Cardiovascular Disease Stroke Chronic Kidney Disease Less << Phase 4 Completed - Spain ... More >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 Less <<
NCT02594410 Hypertension Phase 4 Completed - China ... More >> Fuwai Hospital Beijing, China Less <<
NCT02415192 - Unknown November 2016 Korea, Republic of ... More >> LG Life Science Recruiting Seoul, Jongno gu, Korea, Republic of, 110-783 Contact: Hye jin Yoon Less <<
NCT03195023 Renal Insufficiency, Chronic ... More >> Proteinuria Less << Phase 4 Recruiting June 2021 Spain ... More >> Gregorio Maranon Hospital Recruiting Madrid, Spain, 28007 Contact: Maria Angeles Goicoechea, PhD, MD    0034609838684    marian.goicoechea@gmail.com    Contact: Ana María García, MD    0034676611045    anamgarciaprieto@gmail.com Less <<
NCT01211314 Hypertension Phase 4 Terminated(sponsor decision) - Israel ... More >> Clalit Health Services Hertsliyah, Hasharon, Israel Less <<
NCT01180413 Essential Hypertension ... More >> High Blood Pressure Less << Phase 4 Completed - Denmark ... More >> Aarhus University Hospital - dept. cardiology (A) Aarhus, Denmark, 8000 Less <<
NCT01093807 Essential Hypertension Phase 2 Completed - France ... More >> Hôpital de la Pitié-Salpétrière Paris, France Less <<
NCT00160498 Hypertension COMPLETED 2025-08-05 -
NCT01928628 Hypertension Phase 3 Completed - Korea, Republic of ... More >> Seoul National University Hospital Seoul, Korea, Republic of Less <<
NCT01122251 Essential Hypertension Phase 2 Completed - Korea, Republic of ... More >> 23 sites in Korea Seoul, Busan etc., Korea, Republic of Seoul National University Hospital Seoul, Korea, Republic of Less <<
NCT01520285 Hypertension Phase 4 Completed - China ... More >> Shanghai First People's Hospital Shanghai, China, 200000 Less <<
NCT03497156 Obesity, Morbid RECRUITING 2025-10-26 St. Olavs University Hospital,... More >> Trondheim, Norway Less <<
NCT00564057 HIV Infections ... More >> Hypertension Less << Phase 4 Unknown September 2009 Italy ... More >> University of Insubria, Department of Clinical Medicine Recruiting Varese, Italy, 21100 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.63mL

0.33mL

0.16mL

8.17mL

1.63mL

0.82mL

16.35mL

3.27mL

1.63mL

References

 

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