Candesartan

For research use only. Not for therapeutic Use.

  • CAT Number: A000781
  • CAS Number: 139481-59-7
  • Molecular Formula: C24H20N6O3
  • Molecular Weight: 440.45
  • Purity: ≥95%
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Candesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Candesartan is marketed as the cyclohexyl 1-hydroxyethyl carbonate (cilexetil) ester, known as candesartan cilexetil. Candesartan cilexetil is metabolised completely by esterases in the intestinal wall during absorption to the active candesartan moieity. The use of a prodrug form increases the bioavailability of candesartan. Despite this, absolute bioavailability is relatively poor at 15% (candesartan cilexetil tablets) to 40% (candesartan cilexetil solution). Its IC50 is 15 μg/kg.


Catalog Number A000781
CAS Number 139481-59-7
Synonyms

139481-59-7; Blopress; Ratacand; 1-((2/’-(1H-Tetrazol-5-yl)-[1,1/’-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid; CV-11974

Molecular Formula C24H20N6O3
Purity ≥95%
Target Vitamin D Related/Nuclear Receptor
Solubility >14.7mg/mL in DMSO
Storage -20°C
InChI 1S/C24H20N6O3/c1-2-33-24-25-20-9-5-8-19(23(31)32)21(20)30(24)14-15-10-12-16(13-11-15)17-6-3-4-7-18(17)22-26-28-29-27-22/h3-13H,2,14H2,1H3,(H,31,32)(H,26,27,28,29)
InChIKey HTQMVQVXFRQIKW-UHFFFAOYSA-N
SMILES CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O
Reference

1: Krishna MV, Sowhardhra M, Kumar MS, Madhavi G, Jadhav T, Thakkar D. Effect of
surfactants and hydrophilic polymers on the stability of an antihypertensive drug
candesartan cilexetil: Evaluation by HPLC. Ann Pharm Fr. 2017 Nov 22. pii:
S0003-4509(17)30036-6. doi: 10.1016/j.pharma.2017.09.001. [Epub ahead of print]
PubMed PMID: 29174608.
<br>

2: Heck SL, Gulati G, Hoffmann P, von Knobelsdorff-Brenkenhoff F, Stor&#229;s TH, Ree
AH, Gravdehaug B, R&#248;sj&#248; H, Steine K, Geisler J, Schulz-Menger J, Omland T. Effect
of candesartan and metoprolol on myocardial tissue composition during
anthracycline treatment: the PRADA trial. Eur Heart J Cardiovasc Imaging. 2017
Jun 29. doi: 10.1093/ehjci/jex159. [Epub ahead of print] PubMed PMID: 29106497.
<br>

3: Murad HA, Gazzaz ZJ, Ali SS, Ibraheem MS. Candesartan, rather than losartan,
improves motor dysfunction in thioacetamide-induced chronic liver failure in
rats. Braz J Med Biol Res. 2017 Sep 21;50(11):e6665. doi:
10.1590/1414-431X20176665. PubMed PMID: 28953991; PubMed Central PMCID:
PMC5609604.
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4: 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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5: 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>

6: Bessaguet F, Danigo A, Magy L, Sturtz F, Desmoulière A, Demiot C. Candesartan
prevents resiniferatoxin-induced sensory small-fiber neuropathy in mice by
promoting angiotensin II-mediated AT2 receptor stimulation. Neuropharmacology.
2017 Nov;126:142-150. doi: 10.1016/j.neuropharm.2017.08.039. Epub 2017 Sep 5.
PubMed PMID: 28882562.
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7: Lammel-Lindemann JA, Flores-Villalba E, Martagón AJ, DeObeso-Gonzalez E,
Puente-Gallegos F. Noncholestatic acute hepatocellular injury following
candesartan administration. Br J Clin Pharmacol. 2017 Aug 25. doi:
10.1111/bcp.13406. [Epub ahead of print] PubMed PMID: 28841231.
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8: Lyamin NP, Nalivayeva AV, Mordwintseva AY. [Candesartan is the Basis of
Therapy for Arterial Hypertension in Middle-Aged Women]. Kardiologiia. 2017
May;57(5):62-67. Russian. PubMed PMID: 28762923.
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9: Sohn IS, Kim CJ, Ahn T, Youn HJ, Jeon HK, Ihm SH, Cho EJ, Chung WB, Chae SC,
Kim WS, Nam CW, Park SM, Choi JY, Kim YK, Hong TJ, Lee HY, Cho JH, Shin ES, Yoon
JH, Yang TH, Jeong MH, Lee JH, Park JI. Efficacy and Tolerability of Combination
Therapy Versus Monotherapy with Candesartan and/or Amlodipine for Dose Finding in
Essential Hypertension: A Phase II Multicenter, Randomized, Double-blind Clinical
Trial. Clin Ther. 2017 Aug;39(8):1628-1638. doi: 10.1016/j.clinthera.2017.06.014.
Epub 2017 Jul 19. PubMed PMID: 28734660.
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10: Kabel AM, Elkhoely AA. Ameliorative Effect of Coenzyme Q10 and/or Candesartan
on Carboplatin-Induced Nephrotoxicity: Roles of Apoptosis, Transforming Growth
Factor-Β1, Nuclear Factor Kappa-B And The Nrf2/HO-1 Pathway. Asian Pac J Cancer
Prev. 2017 Jun 25;18(6):1629-1636. PubMed PMID: 28670881.

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