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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
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 610.66
Formula C33H34N6O6
CAS Number 145040-37-5
Purity >99%
Solubility DMSO 52 mg/mL
Storage at -20°C
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

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