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Art. -Nr.: HY-12502C

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(R)-Efonidipine

Name: (R)-Efonidipine
Brand: MedChemExpress
SKU: HY-12502C
Availability: PreOrder

(Synonyms: (R)-NZ-105; (-)-Efonidipine)

(R)-Efonidipine ((R)-NZ-105) is an orally active, selective T-type Ca²⁺ channel blocker. (R)-Efonidipine does not inhibit high-voltage-activated Ca²⁺ channels, voltage-dependent Na⁺ channels, or Ca²⁺-activated K⁺ channels. (R)-Efonidipine modulates cardiac autonomic function by increasing parasympathetic activity and decreasing sympathetic activity. (R)-Efonidipine significantly improves survival in a mouse model of dilated cardiomyopathy. (R)-Efonidipine can be used in research on ischemic encephalopathy, heart failure, and hypertension.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 128194-13-8
Formel: C₃₄H₃₈N₃O₇P
Molecular Weight:631.66

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (284 KB)

(R)-Efonidipine Chemical Structure

CAS. Nr.: 128194-13-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

T-type calcium channel

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In Vitro

R(−) efonidipine (3 min) selectively inhibits T-type Ba²⁺ currents in dissociated rat hippocampal CA1 pyramidal neurons with an IC₅₀ of 221 μM, without affecting HVA Ba²⁺ currents^[1].
R(−) efonidipine (300 μM) strongly promotes inactivation of T-type Ca²⁺ channels in dissociated rat hippocampal CA1 pyramidal neurons, shifting the inactivation V₀.₅ by 15.4 mV, while only slightly affecting activation^[1].
R(−) efonidipine (300 μM; 180 s) similarly inhibits both T-type Ca²⁺ and Ba²⁺ currents in dissociated rat hippocampal CA1 pyramidal neurons, suppressing them to approximately 53% and 56% of control, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(R)-Efonidipine (200 mg·kg^-1·d^-1; p.o.; for 20 weeks) dramatically improves survival among dnNRSF-Tg mice without significantly affecting blood pressure, heart rate, cardiac structure, or systolic function^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

dnNRSF-Tg transgenic mice (cardiac-specific dominant-negative neuron-restrictive silencer factor transgenic mice)^[2]
Dosage:

200 mg·kg^-1·d^-1
Administration:

p.o.; for 20 weeks
Result:

Did not significantly affect blood pressure, heart rate, cardiac structure, or systolic function in either WT or dnNRSF-Tg mice compared with vehicle.
Dramatically improved the survival rate among dnNRSF-Tg mice.

Related Protocols :

Chemical Information

CAS. Nr. 128194-13-8
Molecular Weight 631.66
Formel C₃₄H₃₈N₃O₇P
SMILES

O=C(C1=C(C)NC(C)=C(P2(OCC(C)(CO2)C)=O)[C@@H]1C3=CC([N+]([O-])=O)=CC=C3)OCCN(C4=CC=CC=C4)CC5=CC=CC=C5
Synonyms

(R)-NZ-105; (-)-Efonidipine
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shin MC, et al. A selective T-type Ca2+ channel blocker R(-) efonidipine. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377(4-6):411-21.

[2]. Kinoshita H, et al. T-type Ca2+ channel blockade prevents sudden death in mice with heart failure. Circulation. 2009 Sep 01;120(9):743-52.

[3]. Furukawa T, et al. Identification of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels. British journal of pharmacology. 2004 Dec;143(8):1050-7.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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(R)-Efonidipine

Alle Calcium Channel Isoform-spezifische Produkte anzeigen