Nitrendipine
Based on 3 publication(s) in Google Scholar
Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 39562-70-4
- Formula: C18H20N2O6
- Molecular Weight:360.36
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Storage:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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FDA-Approved Drug Library
HY-L022
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Anti-Cancer Compound Library
HY-L025
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Drug Repurposing Compound Library
HY-L035
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Ferroptosis Compound Library
HY-L051
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NMPA-Approved Drug Library
HY-L053
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Orally Active Compound Library
HY-L061
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FDA Approved & Pharmacopeial Drug Library
HY-L066
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Neuroprotective Compound Library
HY-L070
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Calcium Channel Blocker Library
HY-L117
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FDA-Approved Anticancer Drug Library
HY-L122
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Human Metabolite Library
HY-L123
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Anti-Aging Natural Product Library
HY-L134
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Off-patent Drug Library
HY-L141
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Antihypertensive Compound Library
HY-L145
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HY-L149
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HY-L150
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HY-L162
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HY-L022P
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FDA-Approved Drug Library Mini
HY-L022M
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Nitrendipine
MoreAll Calcium Channel Isoforms
More
Biological Activity
Calcium channel[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
3.8 μM
Compound: 56
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Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx
Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx
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[PMID: 20356305] |
| CHO | IC50 |
0.03 μM
Compound: nitrendipine
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
| LLC-MK2 | IC50 |
137.72 μM
Compound: Nitrendipine
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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
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[PMID: 20934347] |
| LLC-MK2 | IC50 |
26.88 μM
Compound: Nitrendipine
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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
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[PMID: 20934347] |
| LLC-PK1 | IC50 |
68.2 μM
Compound: Nitrendipine
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 12128170] |
| PC-12 | IC50 |
1 x 10-9M
Compound: nitrendipine
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Ability to block depolarization induced 45Ca uptake into pheochromocytoma PC12 cells
Ability to block depolarization induced 45Ca uptake into pheochromocytoma PC12 cells
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[PMID: 6304312] |
Nitrendipine (25-200 μM; 24-48 h) decreases the proliferation of murine neuroblastoma (N2a cells) in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nitrendipine (25-50 mg/kg; i.p.; once a day during the morphine treatment for chronic study, 1 h after the last dose of morphine for acute study) blocks some signs of Morphine withdrawal in mice, such as hair raising, sniffing, diarrhea and the number of jumps[3].
Nitrendipine (1-10 mg/kg; i.p.; twice-daily) blocks the antinociceptive effects of chronic ethanol and prevents the hyperalgesia produced by ethanol withdrawal in rats[4].
Nitrendipine (50 mg/kg; i.p.) strongly attenuates the lipid peroxidation (LPO) in the lung of mice and rabbits induced by Naphthalene (NAP)[5].
Nitrendipine (10 mg/kg; p.o.; twice a day; 30 days) significantly reduces the right ventricular hypertrophy and pulmonary vascular changes caused by intermittent hypoxia in rats[6].
Nitrendipine (5-10 mg/kg; via catheter of gastric fistula) shows a synergistic effect with Hydrochlorothiazide (HY-B0252) on reducing blood pressure and blood pressure variability in spontaneously hypertensive rats (SHR)[7].
Nitrendipine (1000 ppm; p.o.; 3 weeks) can reduce blood pressure, improve glucose tolerance, and increase glucose uptake in the heart and skeletal muscle of spontaneously hypertensive rats[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (weight: 150-175 g for acute study, 210 g for chronic study; 7-8 wk old), intermittent hypoxia model[6]
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Dosage:10 mg/kg (dissolved in polyethylene glycol 400)
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Administration:For acute study: gavaged, single dose; for chronic study: gavaged, twice a day, 30 days
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Result:Prevented the acute increase in right ventricular systolic pressure caused by hypoxia (in acute study).
Significantly reduced the increase in hematocrit, right ventricular systolic pressure, and right ventricular weight adjusted for body weight (in chronic study).
Reduced the percentage of small pulmonary vessels with muscle and prevented the increase in vessel wall thickness.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 39562-70-4
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Appearance Solid
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Molecular Weight 360.36
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Formula C18H20N2O6
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Color Light yellow to green yellow
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SMILES
O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OCC
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Synonyms
BAY-E-5009
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci China Life Sci
2025 Feb 20. PMID: 39985646 -
Cell Calcium
Mutations and clinical significance of calcium voltage-gated channel subunit alpha 1E (CACNA1E) in non-small cell lung cancer. [Abstract]2022 Mar:102:102527. PMID: 35026540 -
Toxicon
Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]2026 Jan:269:108660. PMID: 41241198
Solvent & Solubility
DMSO : 50 mg/mL (138.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.94 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[2]. Watson WP, et al. The differential effects of felodipine and nitrendipine on cerebral dihydropyridine binding ex vivo and the ethanol withdrawal syndrome in mice. Br J Pharmacol. 1994 Aug;112(4):1017-24. [Content Brief]
[4]. Gatch MB. Nitrendipine blocks the nociceptive effects of chronically administered ethanol. Alcohol Clin Exp Res. 2002 Aug;26(8):1181-7. [Content Brief]
[6]. Michael JR, et al. Nitrendipine attenuates the pulmonary vascular remodeling and right ventricular hypertrophy caused by intermittent hypoxia in rats. Am Rev Respir Dis. 1986 Mar;133(3):375-9. [Content Brief]
[7]. Han P, et al. Synergism of hydrochlorothiazide and nitrendipine on reduction of blood pressure and blood pressure variability in spontaneously hypertensive rats. Acta Pharmacol Sin. 2006 Dec;27(12):1575-9. [Content Brief]
[8]. M Bursztyn, et al. Nitrendipine improves glucose tolerance and deoxyglucose uptake in hypertensive rats. Hypertension. 1994 Jun;23(6 Pt 2):1051-3. [Content Brief]
[9]. He-Hui Xie, et al. Synergism of atenolol and nitrendipine on hemodynamic amelioration and organ protection in hypertensive rats. J Hypertens. 2005 Jan;23(1):193-201. [Content Brief]
[10]. S Kazda, et al. Diuretic effect of nitrendipine contributes to its antihypertensive efficacy: a review. J Cardiovasc Pharmacol. 1988;12 Suppl 4:S1-5. [Content Brief]
[11]. Bellemann, P., et al., [3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity to cardiac membranes. Arzneimittelforschung, 1981. 31(12): p. 2064-7. [Content Brief]
Complete Stock Solution Preparation Table
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 (protect from light). 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 | 2.7750 mL | 13.8750 mL | 27.7500 mL | 69.3751 mL |
| 5 mM | 0.5550 mL | 2.7750 mL | 5.5500 mL | 13.8750 mL | |
| 10 mM | 0.2775 mL | 1.3875 mL | 2.7750 mL | 6.9375 mL | |
| 15 mM | 0.1850 mL | 0.9250 mL | 1.8500 mL | 4.6250 mL | |
| 20 mM | 0.1388 mL | 0.6938 mL | 1.3875 mL | 3.4688 mL | |
| 25 mM | 0.1110 mL | 0.5550 mL | 1.1100 mL | 2.7750 mL | |
| 30 mM | 0.0925 mL | 0.4625 mL | 0.9250 mL | 2.3125 mL | |
| 40 mM | 0.0694 mL | 0.3469 mL | 0.6938 mL | 1.7344 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3875 mL | |
| 60 mM | 0.0463 mL | 0.2313 mL | 0.4625 mL | 1.1563 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3469 mL | 0.8672 mL | |
| 100 mM | 0.0278 mL | 0.1388 mL | 0.2775 mL | 0.6938 mL |
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