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Candesartan Cilexetil

Cat. No. M3570
Candesartan Cilexetil Structure
Synonym:

TCV-116

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
100mg USD 25  USD25 In stock
500mg USD 50  USD50 In stock
1g USD 80  USD80 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 610.66
Formula C33H34N6O6
CAS Number 145040-37-5
Solubility (25°C) DMSO 52 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] Narendar Dudhipala, et al. Candesartan cilexetil loaded nanodelivery systems for improved oral bioavailability

[2] Febry Ardiana, et al. Candesartan cilexetil

[3] Alexander Joost, et al. Candesartan cilexetil: an update

[4] Sheridan M Hoy, et al. Candesartan cilexetil: in children and adolescents aged 1 to <17 years with hypertension

[5] Greg L Plosker, et al. Candesartan cilexetil: a pharmacoeconomic review of its use in chronic heart failure and hypertension

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Keywords: Candesartan Cilexetil, TCV-116 supplier, ATM/ATR, inhibitors, activators

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