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Substance Name: Candesartan cilexetil [USAN]
RN: 145040-37-5
UNII: R85M2X0D68
InChIKey: GHOSNRCGJFBJIB-UHFFFAOYSA-N

Note

  • A prodrug which is metabolized to an active form (CV-11974) to exert its biological effects.

Molecular Formula

  • C33-H34-N6-O6

Molecular Weight

  • 610.6676
 

Classification Codes

  • Angiotensin II Type 1 Receptor Blockers
  • Angiotensin Receptor Antagonists
  • Antagonist (Angiotensin II Receptor)
  • Antihypertensive
  • Antihypertensive Agents
  • Cardiovascular Agents
  • Drug / Therapeutic Agent
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Names and Synonyms

Name of Substance

  • Candesartan cilexetil
  • Candesartan cilexetil [USAN]

Synonyms

  • (+-)-1-Hydroxyethyl 2-ethoxy-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)-7-benzimidazolecarboxylate, cyclohexyl carbonate (ester)
  • Amias
  • Atacand
  • Blopress
  • Candesartan cilexetil
  • Kenzen
  • Parapres
  • TCV-116
  • UNII-R85M2X0D68

Systematic Names

  • 1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, 1-(((cyclohexyloxy)carbonyl)oxy)ethyl ester, (+-)-
  • 1H-Benzimidazolium, 7-carboxy-1-(2-((cyclohexylcarbonyl)oxy)ethyl)-2-ethoxy-1-(2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)-, hydroxide, inner salt, (+-)-

Registry Numbers

CAS Registry Number

  • 145040-37-5

FDA UNII

  • R85M2X0D68

System Generated Number

  • 0145040375

Structure Descriptors

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

CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc4ccc(cc4)c5ccccc5c6nnn[nH]6

Toxicity

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
dog LD50 oral > 2gm/kg (2000mg/kg)   Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 42, Pg. 406, 2000.
mouse LD50 intraperitoneal 807mg/kg (807mg/kg) LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)
Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,
mouse LD50 oral > 2gm/kg (2000mg/kg)   Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,
rat LD50 intraperitoneal 940mg/kg (940mg/kg) BEHAVIORAL: MUSCLE WEAKNESS

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,
rat LD50 oral > 2gm/kg (2000mg/kg)   Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,