Selective angiotensin II receptor antagonist
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Telmisartan

Item No. 11615

Technical Information
Formal Name
4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid
CAS Number
144701-48-4
Synonyms
  • BIBR 277
  • Micardis
  • Pritor
Molecular Formula
C33H30N4O2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 1.6 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 1 mg/ml
λmax
225, 297 nm
SMILES
CC1=CC(C2=NC3=C(C=CC=C3)N2C)=CC4=C1N=C(CCC)N4CC5=CC=C(C6=CC=CC=C6C(O)=O)C=C5
InChi Code
InChI=1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)
InChi Key
RMMXLENWKUUMAY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Angiotensin II is a peptide hormone which regulates blood pressure and fluid balance, contributing to hypertension, atherosclerosis, left ventricular hypertrophy, myocardial infarction, and heart failure.1 Telmisartan is a nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (Ki = 3.7 nM).2 It also acts as a partial agonist of PPARγ, activating the receptor to 25-30% of that produced by the full agonist rosiglitazone (EC50 = 4.5 μM).3 Through these actions, telmisartan potently reduces blood pressure in various animal models of hypertension, diminishing cardiac hypertrophy, cardiovascular and renal risk, and glomerulosclerosis.4,5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Frampton, J.E. Telmisartan: A review of its use in cardiovascular disease prevention. Drugs 71(6), 651-677 (2011).

    2. Wienen, W., Hauel, N., Van Meel, J.C.A., et alPharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br. J. Pharmacol. 110(1), 245-252 (1993).

    3. Benson, S.C., Pershadsingh, H.A., Ho, C.I., et alIdentification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARγ-modulating activity. Hypertension 43(5), 993-1002 (2004).

    4. McClellan, K.J., and Markham, A. Telmisartan. Drugs 56(6), 1039-1044 (1998).

    5. Jugdutt, B.I. Clinical effectiveness of telmisartan alone or in combination therapy for controlling blood pressure and vascular risk in the elderly. Clin. Interv. Aging 5, 403-416 (2010).

    6. Schmieder, R.E., Bakris, G., and Weir, M.R. Telmisartan in incipient and overt diabetic renal disease. J. Nephrol. 24(3), 263-273 (2011).