A prodrug form of candesartan
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Active Metabolite(s)
9003239Candesartan
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Candesartan Cilexetil

Item No. 10489

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid, 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester
CAS Number
145040-37-5
Synonyms
  • Candesartan M1 Cilexetil
  • TCV-116
Molecular Formula
C33H34N6O6
Formula Weight
610.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 3 mg/ml
λmax
206, 254, 305 nm
SMILES
O=C(OC(C)OC(C1=CC=CC2=C1N(CC3=CC=C(C4=C(C5=NN=NN5)C=CC=C4)C=C3)C(OCC)=N2)=O)OC6CCCCC6
InChi Code
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)
InChi Key
GHOSNRCGJFBJIB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    500 mg

    $83

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    1 g

    $158

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    5 g

    $660

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    10 g

    $990

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    Product Description

    Candesartan cilexetil is a prodrug form of the angiotensin II type 1 receptor (AT1) antagonist candesartan (Item No. 9003239).1 Candesartan cilexetil is converted to candesartan by hydrolysis in the gastrointestinal tract.2 It inhibits the pressor response induced by angiotensin II in normotensive rats (ID50 = 0.069 mg/kg), as well as decreases blood pressure, but not heart rate, in spontaneously hypertensive and two kidney-one clip (2K-1C) and 1K-1C renal hypertensive rats (ED25s = 0.68, 0.03, and 0.23 mg/kg, respectively).1,3 Candesartan cilexetil (0.1 mg/kg) reduces stroke incidence and urinary protein excretion in stroke-prone spontaneously hypertensive rats.4 It prevents stress-induced tyrosine hydroxylase transcription and increases AT2 receptor expression in the ventrolateral thalamic nucleus in cold-restraint stressed spontaneously hypertensive rats when administered at a dose of 10 mg/kg per day.5 Formulations containing candesartan cilexetil have been used in the treatment of hypertension and heart failure.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shibouta, Y., Inada, Y., Ojima, M., et al. Pharmacological profile of a highly potent and long-acting angiotensin II receptor antagonist, 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4- yl]methyl]-1H-benzimidazole-7-carboxylic acid (CV-11974), and its prodrug, (+/-)-1-(cyclohexyloxycarbonyloxy)-ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5- yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate (TCV-116). J. Pharmacol. Exp. Ther. 266(1), 114-120 (1993).

    2. Gavras, H. Update on the clinical pharmacology of candesartan cilexetil. Am. J. Hypertens. 13(1 Pt.2), 25S-30S (2000).

    3. Inada, Y., Wada, T., Shibouta, Y., et al. Antihypertensive effects of a highly potent and long-acting angiotensin II subtype-1 receptor antagonist, (+-)-1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H- benzimidazole-7-carboxylate (TCV-116), in various hypertensive rats. J. Pharmacol. Exp. Ther. 268(3), 1540-1547 (1993).

    4. Inada, Y., Wade, T., Ojima, M., et al. Protective effects of candesartan cilexetil (TCV-116) against stroke, kidney dysfunction and cardiac hypertrophy in stroke-prone spontaneously hypertensive rats. Clin. Exp. Hypertens. 19(7), 1079-1099 (1997).

    5. Bregonzio, C., Seltzer, A., Armando, I., et al. Angiotensin II AT1 receptor blockade selectively enhances brain AT2 receptor expression, and abolishes the cold-restraint stress-induced increase in tyrosine hydroxylase mRNA in the locus coeruleus of spontaneously hypertensive rats. Stress 11(6), 457-466 (2008).