Biological Activity
L-type Ca2+ channel blocker and α1A-adrenoceptor antagonist; less active enantiomer. (S)-(+)-Niguldipine hydrochloride (Cat. No. 1123) also available.
Technical Data
| M. Wt | 646.18 |
| Formula | C36H39N3O6.HCl |
| Storage | Desiccate at -20°C |
| CAS Number | 113145-70-3 |
| PubChem ID | 16219720 |
| InChI Key | MHOSUIMBPQVOEU-WAQYZQTGSA-N |
| Smiles | O=C(OC)C1=C(C)NC(C)=C(C(OCCCN3CCC(C4=CC=CC=C4)(C5=CC=CC=C5)CC3)=O)[C@@H]1[C@]2=CC=CC([N+]([O-])=O)=C2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 10 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 646.18. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.55 mL | 7.74 mL | 15.48 mL |
| 5 mM | 0.31 mL | 1.55 mL | 3.1 mL |
| 10 mM | 0.15 mL | 0.77 mL | 1.55 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
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References
References are publications that support the products' biological activity.
Boer et al (1989) (+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha1-adrenoceptor. Eur.J.Pharmacol. 172 131 PMID: 2548881
Graziadei et al (1989) Stereoselective binding of niguldipine enantiomers to alpha1A-adrenoceptors labeled with [3H]5-methyl-urapidil. Eur.J.Pharmacol. 172 329 PMID: 2555206
Hollt et al (1992) Stereoisomers of calcium antagonists which differ markedly in their potencies as calcium blockers are equally effective in modulating drug transport by P-glycoprotein. Biochem.Pharmacol. 43 2601 PMID: 1352973
Wetzel et al (1995) Discovery of alpha1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. J.Med.Chem. 38 1579 PMID: 7752182
Keywords: (R)-(-)-Niguldipine hydrochloride, supplier, Ca2+, channel, blocker, α1-adrenoceptor, alpha1-adrenoceptor, a1-adrenoceptor, a1-adrenergic, α1-adrenergic, alpha1-adrenergic, Receptors, Calcium, CaV, Channels, L-Type, voltage-gated, voltage-dependent, Adrenergic, Alpha-1, Receptors, Voltage-gated, Calcium, Channels, Adrenergic, Alpha-1, Receptors, Tocris Bioscience
