Efonidipine hydrochloride monoethanolate

Discontinued Product

3733 has been discontinued.

View all Ca<sub>V</sub>1.x Channels (L-type) products.
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

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.

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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