(+)-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.
For research use only. We do not sell to patients.
- CAS No.: 113165-32-5
- Formula: C36H39N3O6
- Molecular Weight:609.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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α1-adrenergic receptor 78 nM (Ki) |
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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 |
(+)-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.
Chemical Information
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CAS No. 113165-32-5
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Molecular Weight 609.71
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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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