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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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E413204-25mg | 25mg | In stock | $343.90 | |
E413204-100mg | 100mg | In stock | $1,029.90 | |
E413204-500mg | 500mg | In stock | $3,089.90 |
Calcium Channel Inhibitors
Synonyms | Efonidipine|111011-63-3|Efonidipine [INN]|40ZTP2T37Q|DTXSID9043988|Efonidipine (INN)|NCGC00182046-01|NZ-105|2-(Benzyl(phenyl)amino)ethyl 5-(5,5-dimethyl-2-oxido-1,3,2-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate|2 |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | CHANNEL BLOCKER |
Mechanism of action | Channel blocker of Ca v3.2 |
Product Description | Information Efonidipine Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal. Targets T-type calcium channel In vitro Although efonidipine is not a specific T-type calcium channe (TTCC) blocker as it could also block L-type calcium channe (LTCC), its efficacy in blocking TTCC is much greater than that of LTCC. Efonidipine exerts an inhibitory effect on aldosterone synthesis and secretion in a human adrenocortical cell line (H295R), an effect that is mediated, at least in part, by suppression of 11-β-hydroxylase and aldosterone synthase expression. Efonidipine also suppresses both Ang II- and K+-induced aldosterone secretion, but it blocks the latter at much lower concentrations than the former. In vivo Efonidipine could provide broader beneficial effects including the heart, liver, and plasma, and antioxidant in iron-overload condition in both WT(muβ+⁄+) and HT(muβth-3 ⁄+,) mice. Cell Research(from reference) Cell lines:The NCI-H295R human adrenocortical cell line (H295) Concentrations:0.3 μM and 3 μM Incubation Time:24 h |
ALogP | 4.956 |
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HBD Count | 1 |
Rotatable Bond | 11 |
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IUPAC Name | 2-(N-benzylanilino)ethyl 5-(5,5-dimethyl-2-oxo-1,3,2λ5-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate |
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INCHI | InChI=1S/C34H38N3O7P/c1-24-30(33(38)42-19-18-36(28-15-9-6-10-16-28)21-26-12-7-5-8-13-26)31(27-14-11-17-29(20-27)37(39)40)32(25(2)35-24)45(41)43-22-34(3,4)23-44-45/h5-17,20,31,35H,18-19,21-23H2,1-4H3 |
InChi Key | NSVFSAJIGAJDMR-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C(C(=C(N1)C)P2(=O)OCC(CO2)(C)C)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OCCN(CC4=CC=CC=C4)C5=CC=CC=C5 |
Isomeric SMILES | CC1=C(C(C(=C(N1)C)P2(=O)OCC(CO2)(C)C)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OCCN(CC4=CC=CC=C4)C5=CC=CC=C5 |
PubChem CID | 119171 |
Molecular Weight | 631.66 |
PubChem CID | 119171 |
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CAS Registry No. | 111011-63-3 |
ChEMBL Ligand | CHEMBL2074922 |
ChEBI | CHEBI:146221 |
DrugBank Ligand | DB09235 |
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Lot Number | Certificate Type | Date | Item |
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G2203303 | Certificate of Analysis | Jun 05, 2022 | E413204 |
G2203305 | Certificate of Analysis | Jun 05, 2022 | E413204 |
G2203306 | Certificate of Analysis | Jun 05, 2022 | E413204 |
Solubility | Solubility (25°C) In vitro DMSO: 100 mg/mL (158.31 mM); Ethanol: 40 mg/mL (63.32 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 100 |
DMSO(mM) Max Solubility | 158.3130165 |
1. Tanaka H, Shigenobu K. (2002) Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels.. Cardiovasc Drug Rev, 20 (1): (81-92). [PMID:12070536] |