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Chemical Structure| 63675-72-9 Chemical Structure| 63675-72-9

Structure of Nisoldipine
CAS No.: 63675-72-9

Chemical Structure| 63675-72-9

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Nisoldipine is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

Synonyms: BAY-k 5552; (±)-Nisoldipine; Nisoldipine, Bay K 5552, Sular, Baymycard, Nisocor, Syscor

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Product Details of Nisoldipine

CAS No. :63675-72-9
Formula : C20H24N2O6
M.W : 388.41
SMILES Code : O=C(C1=C(C)NC(C)=C(C(OCC(C)C)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
Synonyms :
BAY-k 5552; (±)-Nisoldipine; Nisoldipine, Bay K 5552, Sular, Baymycard, Nisocor, Syscor
MDL No. :MFCD00478055
InChI Key :VKQFCGNPDRICFG-UHFFFAOYSA-N
Pubchem ID :4499

Safety of Nisoldipine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H332
Precautionary Statements:P501-P261-P264-P280-P302+P352+P312-P304+P340+P312

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

    L-type Cav1.2, IC50:10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Sea urchin sperm 11 μM inhibition of the acrosome reaction Proc Natl Acad Sci U S A. 1985 Mar;82(5):1460-4.
Embryonic stem cell-derived cardiomyocytes (stage 1 and stage 2) 2 μM To investigate the effect of Nisoldipine on intracellular Ca2+ oscillations, results showed that Nisoldipine did not impair Ca2+ oscillations but lowered steady-state Ca2+ levels. Proc Natl Acad Sci U S A. 1999 Jul 6;96(14):8259-64.
Rabbit mesenteric artery smooth muscle cells 50 nM 15 minutes To investigate the inhibitory effect of nisoldipine on single calcium channel activity, results showed that 50 nM nisoldipine almost completely inhibited the activity of both types of calcium channels. Proc Natl Acad Sci U S A. 1986 Aug;83(15):5746-50.
Rabbit coronary artery smooth muscle cells 4x10^-8 M, 1x10^-13 M Nisoldipine inhibited the phasic and tonic contraction responses induced by 128 mM K+ in rabbit coronary artery smooth muscle cells, with IC50 values of 4x10-8 M and 1x10-13 M, respectively. Br J Pharmacol. 1984 Sep;83(1):243-58.
GH3 rat pituitary cells 2 μM 5 minutes Attenuated inward Ca2+ currents by approximately 80% without interfering with other conductances Proc Natl Acad Sci U S A. 1985 Feb;82(4):1108-12.
Rat heart 1 nM to 300 nM 15 or 30 minutes Nisoldipine dose-dependently reduced the efflux of ATP catabolites, with the highest concentration (300 nM) completely suppressing ischemic purine production. Br J Pharmacol. 1984 Dec;83(4):943-9.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Pigs Pentobarbital-anaesthetized pigs Intravenous infusion 0.25, 0.5, 1.0 μg/kg/min Continuous 10-minute infusions To study the effects of nisoldipine on cardiovascular performance and regional blood flow, showing dose-dependent decreases in arterial blood pressure (30%), systemic vascular resistance (30%), and left ventricular filling pressure (15%), but increased heart rate (25%) and LVdP/dt max (20%). Br J Pharmacol. 1986 May;88(1):9-18
Pigs Conscious pig model of myocardial stunning Intravenous infusion 0.5 µg/kg/min Starting 15 min before the first coronary occlusion and ending 30 min after the 10th reperfusion Nisoldipine significantly attenuated myocardial stunning on day 1 but had no effect on late preconditioning on days 2 and 3. J Clin Invest. 1996 Jan 15;97(2):562-76
Pigs Conscious pigs with a fixed chronic coronary artery stenosis Oral 0.24±0.02 mg/kg and 0.47±0.04 mg/kg Two doses, 24 hours apart To study the effects of nisoldipine on regional myocardial blood flow distribution and function in conscious pigs with a fixed coronary artery stenosis. Results showed that nisoldipine did not significantly improve blood flow or function in the post-stenotic myocardium in either group, particularly in animals with severe stenosis. Br J Pharmacol. 1988 May;94(1):219-27
Ferrets Isovolumic coronary-perfused heart model Coronary perfusion 10^-8 M 3 minutes of ischemia followed by 10 minutes of reperfusion To determine the effects of nisoldipine on intracellular calcium concentration and left ventricular function during ischemia and reperfusion. Nisoldipine significantly reduced the ischemia-induced rise in diastolic and systolic intracellular calcium concentration, and lessened the decrease in contractile function. Nisoldipine significantly accelerated the decline in intracellular calcium concentration during reperfusion and improved recovery of contractility and relaxation. These effects were associated with a significant diminution in ischemic lactate production. J Clin Invest. 1992 Jun;89(6):2060-5
Rat Langendorff perfused heart model Perfusion 1 nM to 300 nM Single administration, lasting 15 or 30 minutes Nisoldipine effectively inhibited ATP breakdown during myocardial ischemia, with low doses significantly reducing purine efflux. Br J Pharmacol. 1984 Dec;83(4):943-9.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.75mL

5.15mL

2.57mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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