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Efonidipine

Cat. No. M20441
Efonidipine Structure
Synonym:

NZ-105

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Biological Activity

Efonidipine 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.

Chemical Information
Molecular Weight 631.66
Formula C34H38N3O7P
CAS Number 111011-63-3
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ngoc Minh Nguyen, et al. Biomol Ther (Seoul). Efonidipine Inhibits JNK and NF-κB Pathway to Attenuate Inflammation and Cell Migration Induced by Lipopolysaccharide in Microglial Cells

[2] Rashmi Rajput, et al. J Mol Neurosci. Efonidipine Exerts Cerebroprotective Effect by Down-regulation of TGF-β/SMAD-2-Dependent Signaling Pathway in Diabetic Rats

[3] Suresh Davis, et al. J Cardiovasc Pharmacol. Efonidipine-Induced Exanthematic Drug Eruption and Literature Review

[4] Fuyan Xu, et al. Biochem Biophys Res Commun. Structural basis for efonidipine block of a voltage-gated Ca2+ channel

[5] Hikaru Tanaka, et al. Cardiovasc Drug Rev. Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels

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  Catalog
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Keywords: Efonidipine, NZ-105 supplier, Calcium Channel, inhibitors, activators


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