Cilnidipine

Catalog No.S1293 Synonyms: FRC-8653

Cilnidipine Chemical Structure

Molecular Weight(MW): 492.52

Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.

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Biological Activity

Description Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.
Targets
Calcium channel [1]
In vitro

Cilnidipine (10 mM) suppresses the elevation of the ratio induced by 40 mM KCl, and this suppression is effectively inhibited after the treatment with omega-conotoxin GVIA.[1]

In vivo Cilnidipine reduces Ca(2+) influx via N-type Ca(2+) channels after NMDA receptors activation and then protects neurons against ischemia-reperfusion injury in the rat retina in vivo. [2] Cilnidipine significantly prevents the increase in desmin staining and restores the glomerular podocin and nephrin expression compared with amlodipine in spontaneously hypertensive rat/ND mcr-cp (SHR/ND). Cilnidipine also prevents the increase in renal angiotensin II content, the expression and membrane translocation of NADPH oxidase subunits and dihydroethidium staining in SHR/ND. [3] Cilnidipine (30 mg/kg/d as food admix) treatment suppresses the increase in systolic blood pressure in Dahl salt-sensitive rats. Cilnidipine inhibits the increase in blood urea nitrogen and decrease in creatinine clearance as well as progression of glomerular sclerosis. Cilnidipine reduces plasma norepinephrine level and plasma rennin activity compared with vehicle-treated Dahl S rats. [4] Cilnidipine suppresses the pressor response induced by sympathetic nerve stimulation and angiotensin II in pithed rats. Cilnidipine or omega-conotoxin MVIIA decreases mean blood pressure, but slightly increases heart rate in anesthetized rats. Cilnidipine can affect sympathetic N-type Ca(2+) channels in addition to vascular L-type Ca(2+) channels in antihypertensive doses in the rat in vivo. [5]

Protocol

Solubility (25°C)

In vitro DMSO 99 mg/mL (201.0 mM)
Ethanol 15 mg/mL (30.45 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+corn oil
7mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 492.52
Formula

C27H28N2O7

CAS No. 132203-70-4
Storage powder
Synonyms FRC-8653

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02343250 Completed Hypertension IlDong Pharmaceutical Co Ltd March 2015 Phase 1
NCT02145104 Unknown status Hypertension IlDong Pharmaceutical Co Ltd May 2014 Phase 3
NCT00890279 Unknown status Kidney, Polycystic, Autosomal Dominant Ministry of Health, Labour and Welfare, Japan July 2009 Phase 2
NCT00541853 Unknown status Kidney, Polycystic, Autosomal Dominant Kyorin University|Ministry of Health, Labour and Welfare, Japan December 2007 Phase 4
NCT00325936 Completed Hypertension|Metabolic Syndrome X Boryung Pharmaceutical Co., Ltd July 2005 Phase 4
NCT00325637 Completed Hypertension|Stroke Boryung Pharmaceutical Co., Ltd January 2005 Phase 3

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Calcium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID