(R)-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.
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- No. CAS: 128194-13-8
- Fòrmula: C34H38N3O7P
- Peso molecular:631.66
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
T-type calcium channel |
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:dnNRSF-Tg transgenic mice (cardiac-specific dominant-negative neuron-restrictive silencer factor transgenic mice)[2]
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Dosage:200 mg·kg-1·d-1
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Administration:p.o.; for 20 weeks
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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.
Chemical Information
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No. CAS 128194-13-8
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Peso molecular 631.66
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Fòrmula C34H38N3O7P
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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
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Synonyms
(R)-NZ-105; (-)-Efonidipine
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(R)-Efonidipine Related Classifications
HY-12502C Related Classifications
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Keywords
- (R)-Efonidipine
- 128194-13-8
- (R)-NZ-105
- (-)-Efonidipine
- Calcium Channel
- hippocampal CA1 pyramidal neurons
- T-type α1G Ca2+ channels
- high-voltage-activated Ca2+ channels
- T-type Ca2+ channel blocker
- cardiac autonomic function
- dnNRSF-Tg mice
- ventricular myocytes
- dilated cardiomyopathy
- BHK tk-ts13 cells
- Xenopus oocytes
- Inhibitor
- inhibitor
- inhibit