Cilnidipine (Synonyms: FRC-8653)

Name: Cilnidipine
Brand: MedChemExpress
SKU: HY-17404
Rating: 4.5 (1 reviews)

Cat. No.: HY-17404 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Cilnidipine is a long-acting, second-generation dihydropyridine Ca²⁺-channel blocker on L and N-type Ca²⁺ channel. Antihypertensive effects.

For research use only. We do not sell to patients.

Cilnidipine Chemical Structure

CAS No. : 132203-70-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 32	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 98	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Cilnidipine:

1 Publications Citing Use of MCE Cilnidipine

•J Biochem Mol Toxicol. 2022 Oct 7;e23238. [Abstract]

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Calcium Channel Isoform Specific Products:

View All Isoforms

N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cilnidipine is a long-acting, second-generation dihydropyridine Ca²⁺-channel blocker on L and N-type Ca²⁺ channel^[1]^[2]^[3]^[4]. Antihypertensive effects^[5].

IC₅₀ & Target

L-type calcium channel

Cellular Effect

Cell Line	Type	Value	Description	References
IMR-32	IC₅₀	1.6 μM Compound: Cilnidipine(1)	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	[PMID: 16309909]
LLC-MK2	IC₅₀	221.51 μM Compound: Cilnidipine	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	[PMID: 20934347]
LLC-MK2	IC₅₀	5.62 μM Compound: Cilnidipine	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	[PMID: 20934347]
Oocyte	IC₅₀	12.7 μM Compound: Cilnidipine	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit	[PMID: 22761000]
Oocyte	IC₅₀	5.3 μM Compound: Cilnidipine	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit	[PMID: 22761000]

In Vitro

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.

Cell Viability Assay

Cell Line:	Neuronally differentiated PC12 (nPC12) cells
Concentration:	0, 1, 5, 10, 25, 50, 100, 150, and 200 μM
Incubation Time:	Treated for 2 hours; cell viability was measured after 24 hours
Result:	Cell viability was not affected by low concentrations up to 150 μM, but it was slightly decreased at 200 μM.

Western Blot Analysis

Cell Line:	nPC12 cells
Concentration:	100 μM
Incubation Time:	2 hours
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).

In Vivo

Cilnidipine has potent inhibitory actions on N-type as well as L-type voltage-dependent Ca²⁺-channel in rat dorsal root ganglion neurons^[1].
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.

Animal Model:	Swiss albino mice weighing 25±5 g^[4]
Dosage:	5 and 10 mg/kg
Administration:	administered i.p. 30 min prior to immobilization stress
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.

Clinical Trial

Molecular Weight

492.52

Formula

C₂₇H₂₈N₂O₇

CAS No.

132203-70-4

Appearance

Solid

Color

Light yellow to green yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.72%

Select Batch:

Data Sheet (279 KB) SDS (475 KB)

COA (247 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

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. [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

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

Cilnidipine Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cilnidipine132203-70-4FRC-8653FRC8653FRC 8653Calcium ChannelCa2+ channelsCa channelslong-actingdihydropyridine CachannelAntihypertensiveInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Cilnidipine (Synonyms: FRC-8653)

Customer Review

Other Forms of Cilnidipine:

Cilnidipine Related Antibodies

1 Publications Citing Use of MCE Cilnidipine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Calcium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Cilnidipine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Cilnidipine Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report