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Nisoldipine

Cat. No. M3462
Nisoldipine Structure
Synonym:

BAY-k 5552

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100mg USD 50  USD50 In stock
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Quality Control & Documentation
Biological Activity

Nisoldipine (Sular) is a calcium channel blocker. It works by affecting the movement of calcium into the cells of the heart and blood vessels. As a result, it relaxes blood vessels and increases the supply of blood and oxygen to the heart while reducing its workload . [1, 2]

Protocol (for reference only)
Cell Experiment
Cell lines Ventricular myocytes
Preparation method Bathing the myocytes in normal Tyrode's solution, held at -80 mV, and depolarised after 200-ms prepulses (-40mV) to more positive potentials for 500 ms at 0.1 Hz, recording tail currents on repolarisations to -40mV. Exposing the myocytes to 10-100 mM Nisoldipine for 8-10 minutes. Then using an EPC-7 amplifier to record the whole-cell membrane currents.
Concentrations Dissolved in DMSO, final concentration 10-100 μM
Incubation time 8-10 minutes
Animal Experiment
Animal models Male Wistar rats with chronic intragastric ethanol exposure
Formulation Dissolved in DMSO and diluted in saline
Dosages 10 mg/kg
Administration Oral every day
Chemical Information
Molecular Weight 388.41
Formula C20H24N2O6
CAS Number 63675-72-9
Solubility (25°C) DMSO 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] R Heinig. Clinical pharmacokinetics of nisoldipine coat-core

[2] H D Langtry, et al. Nisoldipine coat-core. A review of its pharmacodynamic and pharmacokinetic properties and clinical efficacy in the management of ischaemic heart disease

[3] J Langan, et al. Nisoldipine CC: clinical experience in hypertension

[4] G L Plosker, et al. Nisoldipine coat-core. A review of its pharmacology and therapeutic efficacy in hypertension

[5] A Knorr. The pharmacology of nisoldipine

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  Catalog
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Keywords: Nisoldipine, BAY-k 5552 supplier, Calcium Channel, inhibitors, activators


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