Manidipine 2HCl
Catalog No.S2482 Synonyms: CV-4093
Molecular Weight(MW): 683.62
Manidipine 2HCl 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.
Purity & Quality Control
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Biological Activity
| Description | Manidipine 2HCl 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. | ||
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| 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] |
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| 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] |
Protocol
| Cell Research:[4] |
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| Animal Research:[5] |
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Solubility (25°C)
| In vitro | DMSO | 21 mg/mL (30.71 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents individually and in order: 2% DMSO+30% PEG 300+ddH2O |
2mg/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 | 683.62 |
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| Formula | C35H38N4O6.2HCl |
| CAS No. | 89226-75-5 |
| Storage | powder |
| Synonyms | CV-4093 |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT00627952 | Completed | Hypertension | University of Erlangen-Nürnberg Medical School|Chiesi Farmaceutici S.p.A. | November 2007 | Phase 3 |
| NCT00157586 | Completed | Type 2 Diabetes | Mario Negri Institute for Pharmacological Research | February 2002 | Phase 3 |
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