Cilnidipine
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MedKoo CAT#: 326734

CAS#: 132203-70-4

Description: Cilnidipine, also known as FRC-8653, is a calcium channel blocker. Cilnidipine is the novel calcium antagonist accompanied with L-type and N-type calcium channel blocking function. It was approved in 1995. Compared with other calcium antagonists, cilnidipine can act on the N-type calcium channel that existing sympathetic nerve end besides acting on L-type calcium channel that similar to most of the calcium antagonists.


Chemical Structure

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Cilnidipine
CAS# 132203-70-4

Theoretical Analysis

MedKoo Cat#: 326734
Name: Cilnidipine
CAS#: 132203-70-4
Chemical Formula: C27H28N2O7
Exact Mass: 492.19
Molecular Weight: 492.528
Elemental Analysis: C, 65.84; H, 5.73; N, 5.69; O, 22.74

Price and Availability

Size Price Availability Quantity
1g USD 250
2g USD 450
5g USD 850
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Synonym: FRC-8653; FRC 8653; FRC8653; Cilnidipine; Atelec; Cinalong; Siscard.

IUPAC/Chemical Name: (E)-Cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate

InChi Key: KJEBULYHNRNJTE-DHZHZOJOSA-N

InChi Code: InChI=1S/C27H28N2O7/c1-18-23(26(30)35-14-8-11-20-9-5-4-6-10-20)25(21-12-7-13-22(17-21)29(32)33)24(19(2)28-18)27(31)36-16-15-34-3/h4-13,17,25,28H,14-16H2,1-3H3/b11-8+

SMILES Code: 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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 492.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Kuwahara K, Kimura T. The organ-protective effect of N-type Ca(2+) channel blockade. Pharmacol Ther. 2015 Jul;151:1-7. doi: 10.1016/j.pharmthera.2015.02.001. Epub 2015 Feb 7. Review. PubMed PMID: 25659931.

2: Ando K. L-/N-type calcium channel blockers and proteinuria. Curr Hypertens Rev. 2013 Aug;9(3):210-8. Review. PubMed PMID: 24479751.

3: Homma K, Hayashi K, Yamaguchi S, Fujishima S, Hori S, Itoh H. Renal microcirculation and calcium channel subtypes. Curr Hypertens Rev. 2013 Aug;9(3):182-6. Review. PubMed PMID: 24479750; PubMed Central PMCID: PMC4033552.

4: Chandra KS, Ramesh G. The fourth-generation Calcium channel blocker: cilnidipine. Indian Heart J. 2013 Dec;65(6):691-5. doi: 10.1016/j.ihj.2013.11.001. Review. PubMed PMID: 24407539; PubMed Central PMCID: PMC3905258.

5: Xu G, Wu H, Du B, Qin L. The efficacy and safety of cilnidipine on mild to moderate essential hypertension: a systematic review and meta-analysis of randomized controlled trials in Chinese patients. Cardiovasc Hematol Disord Drug Targets. 2012 Sep;12(1):56-62. Review. PubMed PMID: 22746347.

6: Hayashi K, Homma K, Wakino S, Tokuyama H, Sugano N, Saruta T, Itoh H. T-type Ca channel blockade as a determinant of kidney protection. Keio J Med. 2010;59(3):84-95. Review. PubMed PMID: 20881449.

7: Ito Y, Araki N. [Calcium antagonists: current and future applications based on new evidence. Neuroprotective effect of calcium antagonists]. Clin Calcium. 2010 Jan;20(1):83-8. doi: CliCa10018388. Review. Japanese. PubMed PMID: 20048438.

8: Mizuta E, Hamada T, Igawa O, Shigemasa C, Hisatome I. [Calcium antagonists: current and future applications based on new evidence. The mechanisms on lowering serum uric acid level by calcium channel blockers]. Clin Calcium. 2010 Jan;20(1):45-50. doi: CliCa10014550. Review. Japanese. PubMed PMID: 20048433.

9: Hirooka Y, Sunagawa K. [Calcium antagonists: current and future applications based on new evidence. Calcium channel blockers and autonomic nervous system]. Clin Calcium. 2010 Jan;20(1):32-7. doi: CliCa10013237. Review. Japanese. PubMed PMID: 20048431.

10: Takahara A. Cilnidipine: a new generation Ca channel blocker with inhibitory action on sympathetic neurotransmitter release. Cardiovasc Ther. 2009 Summer;27(2):124-39. doi: 10.1111/j.1755-5922.2009.00079.x. Review. PubMed PMID: 19426250.

11: Hayashi K, Wakino S, Sugano N, Ozawa Y, Homma K, Saruta T. Ca2+ channel subtypes and pharmacology in the kidney. Circ Res. 2007 Feb 16;100(3):342-53. Review. PubMed PMID: 17307972.

12: Hermida RC, Smolensky MH. Chronotherapy of hypertension. Curr Opin Nephrol Hypertens. 2004 Sep;13(5):501-5. Review. PubMed PMID: 15300155.

13: Suzuki H, Kanno Y. [Diagnosis of and therapy for renal hypertension]. Nihon Naika Gakkai Zasshi. 2004 Mar 10;93(3):488-92. Review. Japanese. PubMed PMID: 15052808.

14: Uneyama H, Takahara A, Wakamori M, Mori Y, Yoshimoto R. Pharmacology of N-type Ca2+ channels distributed in cardiovascular system (Review). Int J Mol Med. 1999 May;3(5):455-66. Review. PubMed PMID: 10202175.

15: Saruta T. Current status of calcium antagonists in Japan. Am J Cardiol. 1998 Nov 12;82(9B):32R-34R. Review. PubMed PMID: 9822142.