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(S)-Propafenone

Cat. No. M14774
(S)-Propafenone Structure
Synonym:

(S)-SA-79

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Biological Activity

(S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity.

Chemical Information
Molecular Weight 341.44
CAS Number 107381-32-8
Solubility (25°C) DMSO 33.33 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] Gregory Y H Lip, et al. Atrial fibrillation

[2] Iouri Bachmakov, et al. Characterisation of (R/S)-propafenone and its metabolites as substrates and inhibitors of P-glycoprotein

[3] P S Wells, et al. Interactions of warfarin with drugs and food

[4] H K Kroemer, et al. Enantiomer/enantiomer interaction of (S)- and (R)-propafenone for cytochrome P450IID6-catalyzed 5-hydroxylation: in vitro evaluation of the mechanism

[5] W Schreibmayer, et al. Stereoselective interactions of (R)- and (S)-propafenone with the cardiac sodium channel

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