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Efonidipine - 99%, high purity , CAS No.111011-63-3, Channel blocker of Ca v3.2

  • Moligand™
  • ≥99%
Item Number
E413204
Grouped product items
SKUSizeAvailabilityPrice Qty
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

View related series
Cav3.2 Channel blocker

Basic Description

SynonymsEfonidipine|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
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsEfonidipine (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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeCHANNEL BLOCKER
Mechanism of actionChannel 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 

Product Properties

ALogP4.956
HBD Count1
Rotatable Bond11

Associated Targets

CACNA1H Tclin Voltage-dependent T-type calcium channel subunit alpha-1H 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABCB1 Tchem Multidrug resistance protein 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

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
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

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3 results found

Lot NumberCertificate TypeDateItem
G2203303Certificate of AnalysisJun 05, 2022 E413204
G2203305Certificate of AnalysisJun 05, 2022 E413204
G2203306Certificate of AnalysisJun 05, 2022 E413204

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 100 mg/mL (158.31 mM); Ethanol: 40 mg/mL (63.32 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility100
DMSO(mM) Max Solubility158.3130165

Related Documents

References

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]

Solution Calculators