Candesartan cilexetil is a specific nonpeptide Ang II receptor (ATR) antagonist and the prodrug of candesartan which is an ATR antagonist with an IC50 of 15 µg/kg. Candesartan cilexetil efficacy is entirely due to its active metabolite candesartan (CV-11794) and is dose-dependent over the range of 1–8 mg and its clinical antihypertensive dose is stated to be around 4 mg/day. Candesartan cilexetil is administered as a pro-drug that undergoes activation during gastrointestinal absorption. In clinical trials, candesartan cilexetil has produced a dose-dependent effect when given in dosages of 2-32 mg/day. Observed trough-to-peak blood pressure ratios support a once-daily dosage regimen. The antihypertensive effect of candesartan cilexetil 4-16 mg/day was as great as that of enalapril 10-20 mg/day and amlodipine 5 mg/day and larger than that of losartan potassium 50 mg/day. Adding candesartan cilexetil to hydrochlorothiazide 12.5-25 mg/day and amlodipine 5 mg/day led to enhanced blood-pressure reductions and was well tolerated.
|Solubility (25°C)||DMSO 52 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related ATM/ATR Products|
ATR-IN-24 is a ATR inhibitor.
ATM inhibitor-6 (A-193) is a selective ATM kinase inhibitor.
ATR-IN-21 is a potent ATR inhibitor with an IC50 value of <1000 nM.
ATR-IN-23 is a potent and selective ATR inhibitor with an IC50 of 1.5 nM.
ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC50 value of 1 nM.
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