Efonidipine hydrochloride monoethanolate

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Cat.No. 3733 - Efonidipine hydrochloride monoethanolate | C34H38N3O7P.HCl.C2H5OH | CAS No. 111011-76-8
Description: CaV1.x and CaV3.x blocker
Chemical Name: 5-(5,5-Dimethyl-2-oxido-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylic acid 2-[phenyl(phenylmethyl)amino]ethyl ester hydrochloride monoethanolate
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

Selective blocker of L-type and T-type Ca2+ channels. Displays minimal inhibition of N- and P/Q-type channels and no inhibition of R-type channels. R(-) and S(+)-enantiomers display different channel selectivity; S(+)-Efonidipine blocks L-type and T-type channels whereas R(-)-Efonidipine displays selectivity for T-type channels. Exhibits antihypertensive activity.

Technical Data

M. Wt 714.18
Formula C34H38N3O7P.HCl.C2H5OH
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 111011-76-8
PubChem ID 163838
InChI Key IKBJGZQVVVXCEQ-UHFFFAOYSA-N
Smiles CC1=C(P4(OCC(C)(C)CO4)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(CC5=CC=CC=C5)C2=CC=CC=C2)=O)=C(C)N1.CCO.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 71.42 100

Preparing Stock Solutions

The following data is based on the product molecular weight 714.18. Batch specific molecular weights may vary from batch to batch due to the degree 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 1.4 mL 7 mL 14 mL
5 mM 0.28 mL 1.4 mL 2.8 mL
10 mM 0.14 mL 0.7 mL 1.4 mL
50 mM 0.03 mL 0.14 mL 0.28 mL

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References

References are publications that support the biological activity of the product.

Masumiya et al (1998) Inhibition of myocardial L- and T-type Ca2+ currents by efonidipine: possible mechanism for its chronotropic effect. Eur.J.Pharmacol. 349 351 PMID: 9671117

Furukawa et al (2004) Identification of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels. Br.J.Pharmacol. 143 1050 PMID: 15545287

Shin et al (2008) A selective T-type Ca2+ channel blocker R(-) efonidipine. Naunyn-Schmied.Arch.Pharmacol. 377 411


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Keywords: Efonidipine hydrochloride monoethanolate, Efonidipine hydrochloride monoethanolate supplier, L-type, T-type, calcium, channels, Ca2+, blockers, inhibitors, inhibits, selective, voltage-gated, voltage-dependent, CaV, Cav1.x, Channels, Cav3.x, 3733, Tocris Bioscience

Citations for Efonidipine hydrochloride monoethanolate

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Literature in this Area

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