Cilnidipine
Based on 4 publication(s) in Google Scholar
Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.
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- Reinheit: 99.89%
- CAS. Nr.: 132203-70-4
- Formel: C27H28N2O7
- Molecular Weight:492.52
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Cilnidipine
MoreAlle Calcium Channel Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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L-type calcium channel |
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Cell Line
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Type | Value | Description | References |
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| IMR-32 | IC50 |
1.6 μM
Compound: Cilnidipine(1)
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Inhibitory activity against N-type calcium channel by calcium influx into IMR32 cells
Inhibitory activity against N-type calcium channel by calcium influx into IMR32 cells
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[PMID: 16309909] |
| IMR-32 | IC50 |
1.6 μM
Compound: 1
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Inhibition of voltage-dependent N-type calcium channel in human IMR32 cells assessed as effect on calcium influx
Inhibition of voltage-dependent N-type calcium channel in human IMR32 cells assessed as effect on calcium influx
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[PMID: 18684623] |
| IMR-32 | IC50 |
1.6 μM
Compound: 1
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Inhibition of Voltage-dependent N-type calcium channel- mediated calcium influx in human IMR-32 cells
Inhibition of Voltage-dependent N-type calcium channel- mediated calcium influx in human IMR-32 cells
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[PMID: 21514827] |
| LLC-MK2 | IC50 |
221.51 μM
Compound: Cilnidipine
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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 |
5.62 μM
Compound: Cilnidipine
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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] |
Cilnidipine inhibits the L-type current with an IC50 of 100 nM in neurons pretreated with omegaCgTx plus omegaAgTx[1].
The IC50 for Cilnidipine in respect of the N-type current is 200 nM[1].
Cilnidipine dose- and time-dependently inhibits Ba2+ currents in A7r5 cells with the IC50 at 10 nM after 10 min[2].
Cilnidipine dose-dependently inhibits depolarization- and Ca2+-induced contractions of rat aortic rings, with an IC50 of 10 nM at 10 min[2].
The viability of nPC12 cells show no significant change up to 150?μM Cilnidipine, but it decreases slightly in the cells treated with greater than 200?μM Cilnidipine[3].
Cilnidipine (100 μM, 2 hours) treatment increases the expression of p85aPI3K p-Akt, p-GSK-3β, and heat shock transcription factor (HSTF-1), and decreases levels of cytosolic cytochrome c, activated caspase 3, and cleaved PARP[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuronally differentiated PC12 (nPC12) cells
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Concentration:0, 1, 5, 10, 25, 50, 100, 150, and 200 μM
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Incubation Time:Treated for 2 hours; cell viability was measured after 24 hours
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Result:Cell viability was not affected by low concentrations up to 150 μM, but it was slightly decreased at 200 μM.
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Cell Line:nPC12 cells
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Concentration:100 μM
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Incubation Time:2 hours
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Result:Increased the IRs of p58a PI3K, p-Akt, p-GSK-3β, and HSTF-1 and decreased the Immunoreactivities (IRs) of cytosolic cytochrome c, activated caspase 3 (17 kDa), and cleaved PARP (85 kDa).
Administration of Cilnidipine (10 mg/kg) and Nimodipine (10 mg/kg) significantly attenuates the immobilized stress-induced behavioral changes and restored memory deficits along with normalization of the corticosterone levels[4].
Cilnidipine and Nimodipine produce comparable beneficial effects in restoring immobilization stress subjected mice[4].
Oral administration of Cilnidipine (3 mg/kg) markedly lowers both systolic and diastolic blood pressure 1 hr after administration in 2K1C renal hypertensive dogs[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss albino mice weighing 25±5 g[4]
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Dosage:5 and 10 mg/kg
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Administration:administered i.p. 30 min prior to immobilization stress
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Result:Cilnidipine (10 mg/kg, i.p.) and nimodipine (10 mg/kg, i.p.) 30 min prior to subjecting immobilization stress resulted in significant attenuation of immobilization stress-induced decrease in locomotor activity.
Administration with Cilnidipine (5 mg/kg, i.p.) and Nimodipine (5 mg/kg, i.p.) did not show any significant effect on the stressed mice.
Administration of Cilnidipine (10 mg/kg, i.p.) and Nimodipine (10 mg/kg, i.p.) in the non-stressed mice, and vehicle in the stressed mice did not modulate locomotor activity in a significant manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 132203-70-4
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Appearance Solid
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Molecular Weight 492.52
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Formel C27H28N2O7
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Color Off-white to light yellow
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SMILES
O=C(C1=C(C)NC(C)=C(C(OC/C=C/C2=CC=CC=C2)=O)C1C3=CC=CC([N+]([O-])=O)=C3)OCCOC
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Synonyms
FRC-8653
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Drug Deliv Transl Res
Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]2025 Oct 29. PMID: 41160380 -
J Biochem Mol Toxicol
An in vivo and in vitro model on the protective effect of cilnidipine on contrast-induced nephropathy via regulation of apoptosis and CaMKⅡ/mPTP pathway. [Abstract]2022 Oct 7;e23238. PMID: 36207783 -
bioRxiv
2025 Nov 21:2025.11.20.689520. PMID: 41332603
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (203.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.08 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, 6 months; -20°C, 1 month (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.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (475 KB)
- English - EN (475 KB)
- Français - FR (475 KB)
- Deutsch - DE (475 KB)
- Norwegian - NO (475 KB)
- Español - ES (475 KB)
- Swedish - SV (475 KB)
- Italian - IT (475 KB)
- Korean - KR (475 KB)
- Portuguese - PT (475 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. S Fujii,et al. Effect of cilnidipine, a novel dihydropyridine Ca2+-channel antagonist, on N-type Ca2+ channel in rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 1997 Mar;280(3):1184-91. [Content Brief]
[2]. Matthias Löhn, et al. Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase C. J Hypertens. 2002 May;20(5):885-93. [Content Brief]
[3]. Young Joo Lee, et al. Cilnidipine mediates a neuroprotective effect by scavenging free radicals and activating the phosphatidylinositol 3-kinase pathway. J Neurochem. 2009 Oct;111(1):90-100. [Content Brief]
[4]. Naresh Kumar, et al. Anti-stress effects of cilnidipine and nimodipine in immobilization subjected mice. Physiol Behav. 2012 Mar 20;105(5):1148-55. [Content Brief]
[5]. A Takahara, et al. [Antihypertensive effects of repeated oral administration of cilnidipine, a novel calcium antagonist, in 2K1C renal hypertensive dogs]. Nihon Yakurigaku Zasshi. 1995 Oct;106(4):279-87. [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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0304 mL | 10.1519 mL | 20.3037 mL | 50.7594 mL |
| 5 mM | 0.4061 mL | 2.0304 mL | 4.0607 mL | 10.1519 mL | |
| 10 mM | 0.2030 mL | 1.0152 mL | 2.0304 mL | 5.0759 mL | |
| 15 mM | 0.1354 mL | 0.6768 mL | 1.3536 mL | 3.3840 mL | |
| 20 mM | 0.1015 mL | 0.5076 mL | 1.0152 mL | 2.5380 mL | |
| 25 mM | 0.0812 mL | 0.4061 mL | 0.8121 mL | 2.0304 mL | |
| 30 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6920 mL | |
| 40 mM | 0.0508 mL | 0.2538 mL | 0.5076 mL | 1.2690 mL | |
| 50 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 60 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 80 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6345 mL | |
| 100 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5076 mL |
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