Cilnidipine (FRC8653)

Alias: FRC-8653; Cilnidipine; Atelec; Cinalong; Siscard; FRC 8653; FRC8653.
Cat No.:V1650 Purity: ≥98%
Cilnidipine (formerly also known as FRC-8653; FRC8653;Atelec; Cinalong; Siscard)is a novel, potent and unique dual L-type and N-type calcium channel blocker (CCB) that was approved as an anti-hypertensive drug in 1995 for high blood pressure treatment.
Cilnidipine (FRC8653) Chemical Structure CAS No.: 132203-70-4
Product category: Sodium Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cilnidipine (formerly also known as FRC-8653; FRC8653; Atelec; Cinalong; Siscard) is a novel, potent and unique dual L-type and N-type calcium channel blocker (CCB) that was approved as an anti-hypertensive drug in 1995 for high blood pressure treatment. Cilnidipine lowers mean blood pressure and reduces the size of cerebral infarction in the rat model of focal brain ischemia. Cilnidipine has displayed renal and vascular protective effects and improved baroreflex sensitivity in patients with hypertension. It has also demonstrated neuroprotective effects in a rat focal brain ischemia model by removing free radicals and activating the phosphatidylinositol 3-kinase pathway.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In neurons pretreated with omegaCgTx plus omegaAgTx, celidipine inhibits the L-type current with an IC50 of 100 nM[1]. Cilnidipine's IC50 with regard to the N-type current is 200 nM[1]. With an IC50 of 10 nM at 10 min, clinidipine dose- and time-dependently inhibits the contractions of rat aortic rings caused by depolarization and Ca2+[2]. When exposed to more than 200 μM of Cilnidipine, the viability of nPC12 cells decreases slightly, but does not change significantly up to 150 μM of the drug[3]. After two hours of treatment at 100 μM, cilnidipine increases the expression of p85aPI3K, p-Akt, p-GSK-3β, and heat shock transcription factor (HSTF-1), while cytosolic cytochrome c, activated caspase 3, and cleaved PARP levels decrease[3].
ln Vivo
In rat dorsal root ganglion neurons, cilnidipine has strong inhibitory effects on both L-type and N-type voltage-dependent Ca2+ channels[1]. The use of 10 mg/kg of cilnidipine and 10 mg/kg of nicodipine greatly reduces the behavioral abnormalities brought on by immobilization stress, restores deficit memories, and normalizes corticosterone levels[4]. Both nicodipine and clonidipine have similar positive effects on immobilized mice under stress[4]. In 2K1C renal hypertensive dogs, oral Cilnidipine (3 mg/kg) significantly reduces both systolic and diastolic blood pressure one hour after administration[5].
Cell Assay
Cell Viability Assay
Cell Types: Neuronally differentiated PC12 (nPC12) cells
Tested Concentrations: 0, 1, 5, 10, 25, 50, 100, 150, and 200 μM
Incubation Duration: Treated for 2 hrs (hours); cell viability was measured after 24 hrs (hours)
Experimental Results: Cell viability was not affected by low concentrations up to 150 μM, but it was slightly diminished at 200 μM.

Western Blot Analysis
Cell Types: nPC12 cells
Tested Concentrations: 100 μM
Incubation Duration: 2 hrs (hours)
Experimental Results: Increased the IRs of p58a PI3K, p-Akt, p-GSK-3β, and HSTF-1 and diminished the Immunoreactivities (IRs) of cytosolic cytochrome c, activated caspase 3 (17 kDa), and cleaved PARP (85 kDa).
Animal Protocol
Animal/Disease Models: Swiss albino mice weighing 25±5 g[4]
Doses: 5 and 10 mg/kg
Route of Administration: administered ip 30 min prior to immobilization stress
Experimental Results: Cilnidipine (10 mg/kg, ip) and nimodipine (10 mg/kg, ip) 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, ip) and Nimodipine (5 mg/kg, ip) did not show any significant effect on the stressed mice. Administration of Cilnidipine (10 mg/kg, ip) and Nimodipine (10 mg/kg, ip) in the non -stressed mice, and vehicle in the stressed mice did not modulate locomotor activity in a significant manner.
References
[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.
[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.
[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.
[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.
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H28N2O7
Molecular Weight
492.52
CAS #
132203-70-4
SMILES
O(C([H])([H])C([H])([H])OC([H])([H])[H])C(C1=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C(C(=O)OC([H])([H])/C(/[H])=C(\[H])/C2C([H])=C([H])C([H])=C([H])C=2[H])C1([H])C1C([H])=C([H])C([H])=C(C=1[H])[N+](=O)[O-])=O
Synonyms
FRC-8653; Cilnidipine; Atelec; Cinalong; Siscard; FRC 8653; FRC8653.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:99 mg/mL (201.0 mM)
Water:<1 mg/mL
Ethanol:15 mg/mL (30.5 mM)
Solubility (In Vivo)
5%DMSO+Corn oil: 7 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0304 mL 10.1519 mL 20.3037 mL
5 mM 0.4061 mL 2.0304 mL 4.0607 mL
10 mM 0.2030 mL 1.0152 mL 2.0304 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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