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Manidipine (Manyper) is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. It is used clinically as an antihypertensive. At a holding potential of −37 mV, manidipine decreased the Ca2+ current at concentrations above 0.1 nM, and abolished it at 100 nM. The voltage-dependent effect of manidipine on the Ca2+ current may explain the weak negative inotropism of manidipine in ventricular muscles, and provide an electrophysiological basis for its vascular selectivity.
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Source | Acta Pharmacol Sin (2007). Figure 5. Manidipine |
| Method | Immunohistochemical staining | |
| Cell Lines | 8-OHdG | |
| Concentrations | 50 μm | |
| Incubation Time | ||
| Results | Manidipine treatment also provided moderate relief of oxidative stress-related DNA injury |
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Source | Acta Pharmacol Sin (2007). Figure 3. Manidipine |
| Method | insulin staining | |
| Cell Lines | β-cell | |
| Concentrations | 50 μm | |
| Incubation Time | 6 weeks | |
| Results | β-cell mass was quite low in the db/db control group, and it was rescued greatly after 6 weeks’ treatment by both candesartan 1 mg/kg and 10 mg/kg |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | stroke-prone spontaneously hypertensive rat |
| Formulation | |
| Dosages | 20 mg/kg |
| Administration | oral |
| Molecular Weight | 610.7 |
| Formula | C35H38N4O6 |
| CAS Number | 89226-50-6 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Calcium Channel Products |
|---|
| KB-R7943 mesylate
KB-R7943 mesylate is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 mM). |
| Cilnidipine
Cilnidipine is a dual L- and N-type calcium channel blocker that displays antihypertensive, sympatholytic and neuroprotective activity. |
| Azelnidipine
Azelnidipine is a novel dihydropyridine derivative, a L-type calcium channel blocker, and an antihypertensive. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects. |
| Catharanthine
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM |
| Cinepazide maleate
Cinepazide maleate is a maleate salt form of cinepazide which is a vasodilator. |
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