(+)-Niguldipine
(+)-Niguldipine is a 1,4-DHP receptor ligand associated with L-type Ca2+ channels (with Ki values of 85 pmol/L in guinea pig skeletal muscle, 140 pmol/L in brain, and 45 pmol/L in heart) as well as an α1-adrenergic receptor ligand (with a Ki value of 78 nmol/L). (+)-Niguldipine shows much higher binding selectivity for α1α-adrenergic receptors than for α1B-adrenergic receptors. (+)-Niguldipine can be used in studies related to hypertension.
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- CAS No.: 113165-32-5
- Formule: C36H39N3O6
- Masse moléculaire:609.71
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Stockage:
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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α1-adrenergic receptor 78 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | Inhibition |
92.98 %
Compound: NIGULDIPINE-(S)-(+)
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
In Vitro
(+)-Niguldipine binds with high and roughly comparable affinity to the 1,4-dihydropyridine receptors associated with L-type Ca2+ channels in the cell membranes of guinea pig skeletal muscle (Ki = 85 pmol/L), brain (Ki = 140 pmol/L) and heart (Ki = 45 pmol/L), and is approximately 40 times more potent than its (-)-enantiomer[1].
(+)-Niguldipine (8-19 different concentrations; 45 min) binds to α1-adrenergic receptors in rat liver cell membranes, with a Ki value of 78 nmol/L, and its potency is comparable to that of its (-)-enantiomer[1].
(+)-Niguldipine (8-19 different concentrations; 45-60 min) binds highly selectively to α1A-adrenergic receptors in rat cerebral cortex cell membranes (relative to α1B-adrenergic receptors), with a selectivity index of 617 against [3H]prazosin and 230 against [125I]HEAT; when using [3H]prazosin, its Kh = 52 pmol/l, and it is over 40 times more potent at the α1A subtype than its (-)-enantiomer[1].
(+)-Niguldipine (variable dose; 20 min incubation) displaces the specific binding of [3H]prazosin to rabbit ventricular myocardial membrane fractions at 23.1% of the binding sites with high affinity (Ki = 64.6 pmol/L), while it exhibits low affinity (Ki = 7.08 nmol/L) for the remaining sites[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 113165-32-5
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Masse moléculaire 609.71
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Formule C36H39N3O6
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SMILES
O=C(C1=C(C)NC(C)=C(C(OC)=O)[C@@H]1C2=CC=CC([N+]([O-])=O)=C2)OCCCN3CCC(C4=CC=CC=C4)(C5=CC=CC=C5)CC3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureté et documentation
Références
[1]. Boer R, et al. (+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1989 May 11;172(2):131-45. [Content Brief]
[2]. Endoh M, et al. Effect of (+)-niguldipine on myocardial alpha 1-adrenoceptors in the rabbit. Eur J Pharmacol. 1992 Nov 17;223(2-3):143-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(+)-Niguldipine Related Classifications
HY-137203 Related Classifications
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