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Chemical Structure| 21829-25-4 Chemical Structure| 21829-25-4

Structure of Nifedipine
CAS No.: 21829-25-4

Chemical Structure| 21829-25-4

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Nifedipine is a calcium channel blocker with high affinity for L-type calcium channels, with an IC50 value of 10 nM. Nifedipine has antihypertensive and antianginal effects and can be used in cardiovascular disease research.

Synonyms: BAY-a-1040; BAY 1040

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Product Citations

Product Citations

Fofie, Christian Kuete ; Granja-Vazquez, Rafael ; Truong, Vincent ; Walsh, Patrick ; Price, Theodore ; Biswas, Swati , et al.

Abstract: Chronic pain is a global health issue, yet effective treatments remain limited due to poor preclinical-to-human translation. To address this, we developed a high-content screening (HCS) platform using hiPSC-derived nociceptors to identify analgesics targeting the peripheral nervous system. These cells, cultured on multi-well microelectrode arrays, achieved nearly 100% active electrodes by week 2, maintaining stable activity for at least 2 weeks. After 28 days, we assessed drug effects on neuronal activity, achieving strong assay performance (robust Z′ > 0.5). Pharmacological tests confirmed responses to key analgesic targets, including ion channels (Nav, Cav, Kv, and TRPV1), receptors (AMPAR and GABA-R), and kinase inhibitors (tyrosine and JAK1/2). Transcriptomic analysis validated target expression, though levels differed from primary human DRG cells. The platform was used to screen over 700 natural compounds, demonstrating its potential for analgesic discovery. This HCS platform facilitates the rapid discovery of uncharacterized analgesics, reducing preclinical-to-human translation failure.

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Product Details of Nifedipine

CAS No. :21829-25-4
Formula : C17H18N2O6
M.W : 346.33
SMILES Code : O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
Synonyms :
BAY-a-1040; BAY 1040
MDL No. :MFCD00057326
InChI Key :HYIMSNHJOBLJNT-UHFFFAOYSA-N
Pubchem ID :4485

Safety of Nifedipine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H351-H361
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Nifedipine

TLR

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
Gastric fundus smooth muscle cells 10 µM Nifedipine was used to block L-type calcium currents to study the electrophysiological properties of gastric fundus smooth muscle cells Int J Mol Sci. 2023 Jan 5;24(2):1082.
HVC X neurons 10 μM Used to block L-type calcium channels to study their effect on neuronal activity. Nat Commun. 2020 Feb 19;11(1):952.
Rat aortic smooth muscle cells 25 nM and 100 nM 30 min To investigate the effect of Nifedipine on Ang II-induced NADPH oxidase activity, results showed that Nifedipine significantly attenuated Ang II-induced NADPH oxidase activity. J Mol Cell Cardiol. 2015 Oct;87:152-9.
Human myometrial smooth muscle cells (PHM1-41) 10 µM 48 h To assess the effect of nifedipine on the contractility of myometrial smooth muscle cells. Results showed that nifedipine inhibited TNF/LPS-induced contraction, maintaining a level of contraction similar to the basal vehicle control conditions at 48 h. Sci Rep. 2023 Apr 6;13(1):5646.
Human myometrial smooth muscle cells (PHM1-41) 10 µM 24 h To assess the effect of nifedipine on the inflammatory response of myometrial smooth muscle cells. Results showed that nifedipine did not reduce TNF or LPS-induced pro-inflammatory cytokine gene expression. Sci Rep. 2023 Apr 6;13(1):5646.
CAFs 2.5 μM 24 h To evaluate the effect of Nifedipine on CAF activated phenotype, results showed that Nifedipine reduced CAF motility and ECM remodeling ability J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
WPMY-1 2.5 μM To evaluate the effect of Nifedipine on inward current in WPMY-1 cells, results showed that Nifedipine significantly reduced the inward current J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
Gastric smooth muscle cells 10 μM 1-2 min Nifedipine was used to block L-type Ca2+ channels to study the effect of ADPN on Ca2+ currents in gastric smooth muscle cells. The results showed that ADPN reduced the amplitude of Ca2+ currents. Int J Mol Sci. 2020 Dec 17;21(24):9617.
LNCaP 70 μM 24 h To study the effects of Nifedipine on prostate cancer cells, the results showed that 635 proteins (12.61%) showed significant differences between the treatment and control groups, including 89 upregulated proteins and 147 downregulated proteins. Cancer Biol Med. 2021 Apr 24;19(1):74–89.
DU145 26.66 ± 19.26 μM 72 h To study the effects of Nifedipine on prostate cancer cells, the results showed that Nifedipine produced dose-dependent antiproliferative effects in DU145 cells. Cancer Biol Med. 2021 Apr 24;19(1):74–89.
MGC-803 20.73 ± 10.10 μM 72 h To study the effects of Nifedipine on gastric cancer cells, the results showed that Nifedipine showed toxicity in the MGC-803 cell line. Cancer Biol Med. 2021 Apr 24;19(1):74–89.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice SFTSV infection model Intragastric administration 100 mg/kg Twice a day for 7 days Benidipine hydrochloride and nifedipine significantly reduced viral loads in spleen and serum, and alleviated SFTSV-induced pathogenesis. Cell Res. 2019 Sep;29(9):739-753.
Mice FVB/N mice Apical administration 10 µmol/L Single dose To evaluate the effect of nifedipine on Ca2+ absorption in the ileum of P14 mice, results showed that nifedipine significantly inhibited Ca2+ absorption. Cell Mol Gastroenterol Hepatol. 2019;8(4):625-642
Mice Awake and freely moving CD-1 male mice Intraperitoneal injection 1 mg/kg Single administration, observed for 5 hours Nifedipine (1 mg/kg) did not significantly alter the basal HR in vehicle-treated mice, and it did not modify the effect provoked by JWH-018 injection. The JWH-018-induced tachyarrhythmias were slightly reduced after nifedipine injection in the last two hours of experiment. Nifedipine slightly reduced basal BR one hour following the treatment, and in JWH-018-pretreated mice, it abolished the reduction of breath rate during the first hour of the experiment. The effect on oxygen saturation subsequent to nifedipine administration did not reveal a difference from the vehicle. However, nifedipine was able to slightly increase oxygen saturation immediately after injection when it was administered after JWH-018. Int J Mol Sci. 2023 Apr 19;24(8):7515
Hph-1 mice Ang II-induced abdominal aortic aneurysm model Oral 5 mg/kg and 20 mg/kg Once daily for 14 days To investigate the effect of Nifedipine on the formation of abdominal aortic aneurysm, results showed that Nifedipine significantly reduced the incidence of AAA and improved eNOS coupling state and NO bioavailability. J Mol Cell Cardiol. 2015 Oct;87:152-9.
Mice LPS-induced preterm birth model Intraperitoneal injection 1 mg/kg or 10 mg/kg Every 24 hours until birth To assess the effect of nifedipine on preventing LPS-induced preterm birth. Results showed that nifedipine was unable to consistently delay preterm birth, although it prolonged pregnancy in some mice. Sci Rep. 2023 Apr 6;13(1):5646.
SCID mice Prostate cancer xenograft model Intratumoral injection 250 μl 5 consecutive days for 2 weeks To evaluate the effect of Nifedipine-treated CAF conditioned medium on prostate cancer xenograft growth, results showed that Nifedipine significantly attenuated tumor growth J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
Male nude mice Prostate cancer xenograft model Intraperitoneal injection 50 mg/kg Daily for 15 days To study the effects of Nifedipine on prostate tumor growth, the results showed that Nifedipine significantly inhibited the growth and proliferation of tumors. Cancer Biol Med. 2021 Apr 24;19(1):74–89.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00137501 Labor, Premature PHASE3 TERMINATED 2025-06-09 American University of Beirut ... More >>Medical Center, Beirut, Lebanon Less <<
NCT00185952 Obstetric Labor, Premature|Ven... More >>ous Thrombosis Less << COMPLETED 2025-08-08 Stanford University School of ... More >>Medicine, Stanford, California, 94305, United States Less <<
NCT02072291 Embryo Implantation PHASE2 UNKNOWN 2025-06-18 Hadassah Medical Organization,... More >> Jerusalem, Israel Less <<
NCT01351428 Pre-Eclampsia|Pregnancy|Hypert... More >>ension Less << COMPLETED 2025-11-12 Mount Sinai Hospital, Toronto,... More >> Ontario, M5G1X5, Canada Less <<
NCT00000102 Congenital Adrenal Hyperplasia PHASE1|PHASE2 COMPLETED - Medical University of South Ca... More >>rolina, Charleston, South Carolina, United States Less <<
NCT02527109 Chronic Anal Fissure PHASE2|PHASE3 COMPLETED 2018-08-22 UMHAT "Sveti Georgi", Internal... More >> Consulting Department, Plovdiv, Bulgaria|"Multiprofile Hospital for Active Treatment - Doverie" AD, Clinic of Gastroenterology, Sofia, 1632, Bulgaria|II MHAT, Internal Clinic, Department of Gastroenterology, Sofia, Bulgaria|MC Health BG EOOD, Sofia, Bulgaria|Multiprofile Hospital for Active Treatment Lulin, Sofia, Bulgaria|MC "New rehabilitation centre'' EOOD, Stara Zagora, Bulgaria|"Multiprofile Regional Hospital for Active Treatment - Dr. St. Cherkezov" AD Department of Gastroenterology, Veliko Tarnovo, 5002, Bulgaria|IMSP Spitalul Clinic Municipal Nr 1, Chisinau, Moldova, Republic of|IMSP Spitalul Clinic Municipal Nr 3 "Sfanta Treime", Chisinau, Moldova, Republic of|IMSP Spitalul Clinic Republican, Chisinau, Moldova, Republic of|Med-Gastr Centrum Medyczne, Lodz, 91-034, Poland|Ambulatorium Medyczne Medical Hair & Esthetic, Lublin, 20-844, Poland|Centrum Innowacyjnych Terapii Sp. z o.o. Oddzia? w Piasecznie, Piaseczno, 05-500, Poland|NZOZ Specjalistyczne Centrum Medyczne Flebo, Wolomin, 05-200, Poland|Pelican Impex SRL, Oradea, Jud. Bihor, 410469, Romania|IRGH, Cluj Napoca, Jud. Cluj, 400162, Romania|Tvm Med Serv Srl, Cluj Napoca, Jud. Cluj, Romania|Institutul Regional de Gastroenterologie si Hepatologie "Prof. Dr. Octavian Fodor", Cluj-Napoca, Jud. Cluj, 400162, Romania|SC Schnelbach Medical Care SRL, Ploiesti, Jud. Prahova, Romania|Spit. Clinic Judetean de Urgenta "Sf. Apostol Andrei" Constanta, Constanta, Judet Constanta, Romania|Dacmed SRL, Ploiesti, Judetul Prahova, Romania|Centrul Medical de Diagnostic si Tratament Ambulator Neomed SRL, Brasov, 500283, Romania|Institutul Clinic Fundeni, Bucharest, 022328, Romania|Centrul Medical Sfanta Vineri SRL, Bucharest, Romania Less <<
NCT02090920 Preterm Labor COMPLETED 2025-04-19 Eskenazi Health, Indianapolis,... More >> Indiana, 46202, United States|IU Health Methodist, Indianapolis, Indiana, 46202, United States Less <<
NCT00244530 Kidney Failure, Chronic|Corona... More >>ry Artery Disease Less << PHASE4 COMPLETED 2025-10-05 Rikshospitalet University Hosp... More >>ital, Oslo, 0027, Norway Less <<
NCT02068404 Preterm Labor PHASE4 UNKNOWN 2025-01-16 Centre Hospitalier Universitai... More >>re Vaudois, Lausanne, Vaud, 1011, Switzerland Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.44mL

2.89mL

1.44mL

28.87mL

5.77mL

2.89mL

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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