Candesartan Cilexetil

  • CAT Number: A000670
  • CAS Number: 145040-37-5
  • Molecular Formula: C33H34N6O6
  • Molecular Weight: 610.7
  • Purity: ≥95%
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Candesartan cilexetil is a prodrug of the potent, long-acting, and selective angiotensin II type 1 receptor (AT1) antagonist, candesartan. It is rapidly hydrolyzed to candesartan during gastrointestinal absorptio. Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is, therefore, independent of the pathways for angiotensin II synthesis. Candesartan has much greater affinity ( > 10,000-fold) for the AT1 receptor than for the AT2 receptor.

Catalog Number A000670
CAS Number 145040-37-5
Molecular Formula

C33H34N6O6

Purity 95%
Target AT1 antagonist
Storage -20°C
InChI 1S/C33H34N6O6/c1-3-42-32-34-28-15-9-14-27(31(40)43-21(2)44-33(41)45-24-10-5-4-6-11-24)29(28)39(32)20-22-16-18-23(19-17-22)25-12-7-8-13-26(25)30-35-37-38-36-30/h7-9,12-19,21,24H,3-6,10-11,20H2,1-2H3,(H,35,36,37,38)
InChIKey GHOSNRCGJFBJIB-UHFFFAOYSA-N
SMILES CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6
Reference

1: Amer AM, Allam AN, Abdallah OY. Comparative Pharmaceutical Evaluation of
Candesartan and Candesartan Cilexetil: Physicochemical Properties, In Vitro
Dissolution and Ex Vivo In Vivo Studies. AAPS PharmSciTech. 2017 Sep 25. doi:
10.1208/s12249-017-0879-x. [Epub ahead of print] PubMed PMID: 28948575.

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2: AboulFotouh K, Allam AA, El-Badry M, El-Sayed AM. Development and in vitro/in
vivo performance of self-nanoemulsifying drug delivery systems loaded with
candesartan cilexetil. Eur J Pharm Sci. 2017 Nov 15;109:503-513. doi:
10.1016/j.ejps.2017.09.001. Epub 2017 Sep 6. PubMed PMID: 28889028.
<br>

3: Sunami E, Nomura K, Nishiyama Y, Katayama Y. Effects of Candesartan Cilexetil
Compared with Amlodipine on Serum Asymmetric Dimethylarginine Levels in the
Chronic Stage of Cerebral Infarction: A Preliminary Study. J Nippon Med Sch.
2016;83(6):272-276. doi: 10.1272/jnms.83.272. PubMed PMID: 28133009.

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4: Dudhipala N, Veerabrahma K. Candesartan cilexetil loaded nanodelivery systems
for improved oral bioavailability. Ther Deliv. 2017 Feb;8(2):79-88. doi:
10.4155/tde-2016-0063. PubMed PMID: 28088883.
<br>

5: Park DB, Jang K, Lee JW, Park CW, Lee BH, Kim MG, Jeon JY. Pharmacokinetic and
bioequivalence study comparing a candesartan cilexetil/rosuvastatin calcium
fixed-dose combination with the concomitant administration of candesartan
cilexetil and rosuvastatin calcium in healthy Korean subjects&#8233;. Int J Clin
Pharmacol Ther. 2017 Mar;55(3):286-294. doi: 10.5414/CP202740. PubMed PMID:
28079517.
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6: Paudel A, Ameeduzzafar, Imam SS, Fazil M, Khan S, Hafeez A, Ahmad FJ, Ali A.
Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In
Vitro and In Vivo Evaluation. Curr Drug Deliv. 2017;14(7):1005-1015. doi:
10.2174/1567201813666161230141717. PubMed PMID: 28034361.

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7: Kjeldsen SE, Dzongowski P, Li N, Wang L, Radlmaier A. Fixed-dose combination
of nifedipine gastrointestinal therapeutic system and candesartan cilexetil in
patients with moderate-to-severe essential hypertension: an open-label, long-term
safety and efficacy study. J Clin Pharm Ther. 2016 Dec;41(6):695-702. doi:
10.1111/jcpt.12451. Epub 2016 Sep 27. PubMed PMID: 27670639.
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8: Patel R, Palmer JL, Joshi S, Di Ció Gimena A, Esquivel F. Pharmacokinetic and
Bioequivalence Studies of a Newly Developed Branded Generic of Candesartan
Cilexetil Tablets in Healthy Volunteers. Clin Pharmacol Drug Dev. 2017
Sep;6(5):492-498. doi: 10.1002/cpdd.321. Epub 2016 Dec 22. PubMed PMID: 27753282.

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9: Surampalli G, Nanjwade BK, Patil PA, Chilla R. Novel tablet formulation of
amorphous candesartan cilexetil solid dispersions involving P-gp inhibition for
optimal drug delivery: in vitro and in vivo evaluation. Drug Deliv. 2016
Sep;23(7):2124-2138. Epub 2014 Jul 31. PubMed PMID: 25080228.

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10: Ertürk AS, Gürbüz MU, Tülü M. The effect of PAMAM dendrimer concentration,
generation size and surface functional group on the aqueous solubility of
candesartan cilexetil. Pharm Dev Technol. 2017 Feb;22(1):111-121. doi:
10.1080/10837450.2016.1219372. Epub 2016 Sep 8. PubMed PMID: 27484586.

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