Home Transmembrane Transporters Calcium Channel inhibitor Manidipine 2HCl For research use only.

Manidipine 2HCl

Synonyms: CV-4093

Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.

Manidipine 2HCl Chemical Structure

Manidipine 2HCl Chemical Structure

CAS: 89226-75-5

Selleck's Manidipine 2HCl has been cited by 3 Publications

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Purity & Quality Control

Batch: Purity: 99.57%
99.57

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Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

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Biological Activity

Description Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.
Targets
Calcium channel [1]
(Guinea-pig single ventricular cells )
2.6 nM
In vitro
In vitro At a holding potential of −37 mV, Manidipine decreases the Ca2+ current at concentrations above 0.1 nM, and abolishes it at 100 nM. [1] Manidipine concentration-dependently inhibits the calcium concentration response curves. Manidipine inhibits coronay artery and renal artery with pIC50 of 9.3 nM and 9.1 nM, respectively. [2] Manidipine partly inhibits sympathetic nerve activity and suppresses the mean arterial pressure response to infused norepinephrine. Manidipine also inhibits aldosterone secretion. Manidipine increases in both urinary calcium and uric acid. [3] In addition, Manidipine, at nanomolar concentrations, is efficacious in modulating gene transcriptions that are involved in proinflammatory changes of mesangial cells. [4]
Cell Research Cell lines Mesangial cells
Concentrations 10 nM
Incubation Time Days 1, 3 and 5
Method The mitogenic effect is measured by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, 1 × 105 quiescent cells is seeded into a 25-mL cell culture bottle and kept in low serum medium (0.1% FCS). On the following day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. The medium is replaced each day, and the cells are counted at days 1, 3 and 5.
In Vivo
In vivo Manidipine (3 mg/kg and 10 mg/kg, p.o.) dose-dependently decreases systolic blood pressure in the three types of hypertensive rats. At the dose of 10 mg/kg, Manidipine decreases the blood pressure to the normotensive level between 1 hour and 3 hours after Manidipine is administered; the antihypertensive effect lasted for at least 8 hours. [5] When Manidipine is administered at 10 μg/kg, the hypotensive action is markedly augmented. [6] Manidipine potently inhibits the Ca inward current, When the potential is at -60 mV. Manidipine consistently inhibits the Ca current evoked by depolarization to 0 mV. However, a low concentration of Manidipine (1-3 nM) enhances the Ca current evoked by the depolarizing pulse of -20 mV, when the membrane potential is held at -80 mV. Inhibition of the Ca current induced by Manidipine develops slowly and over 10 minutes is required to reach the maximum inhibition. [7]
Animal Research Animal Models Normotensive male Wistar-Kyoto rats and male stroke-prone SHR
Dosages 1 mg/kg, 3 mg/kg and 10 mg/kg
Administration Administered via p.o.

Chemical Information & Solubility

Molecular Weight 683.62 Formula

C35H38N4O6.2HCl
CAS No. 89226-75-5 SDF Download Manidipine 2HCl SDF
Smiles CC1=C(C(C(=C(N1)C)C(=O)OCCN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4)C5=CC(=CC=C5)[N+](=O)[O-])C(=O)OC.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (146.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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