A nonpeptide AT1 receptor antagonist
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BIBS39

Item No. 22932

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4'-[[2-butyl-6-[[(cyclohexylamino)carbonyl]amino]-1H-benzimidazol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid
CAS Number
133085-33-3
Molecular Formula
C32H36N4O3
Formula Weight
524.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
225, 295 nm
SMILES
CCCCC1=NC2=CC=C(NC(NC3CCCCC3)=O)C=C2N1CC4=CC=C(C5=CC=CC=C5C(O)=O)C=C4
InChi Code
InChI=1S/C32H36N4O3/c1-2-3-13-30-35-28-19-18-25(34-32(39)33-24-9-5-4-6-10-24)20-29(28)36(30)21-22-14-16-23(17-15-22)26-11-7-8-12-27(26)31(37)38/h7-8,11-12,14-20,24H,2-6,9-10,13,21H2,1H3,(H,37,38)(H2,33,34,39)
InChi Key
OLQFKFSAJNUOPT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $95

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    10 mg

    $158

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    25 mg

    $275

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    Product Description

    BIBS39 is a nonpeptide antagonist of the angiotensin II type 1 (AT1) receptor (Ki = 29 nM in rat lung membranes).1 It is selective for AT1 over AT2 receptors (Ki = 480 nM in isolated rat adrenal medulla), as well as α1-, α2-, β1-, and β2-adrenergic, adenosine A1 and A2, muscarinic M1, M2, and M3, and atrial natriuretic peptide receptors (Kis = >100 µM for all). BIBS39 (0.3-10 mg/kg) decreases diastolic blood pressure in pithed normotensive rats without affecting heart rate and in renal hypertensive rats with an increase in heart rate when administered at doses ranging from 1 to 30 mg/kg.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, J., Entzeroth, M., Wienen, W., et al. Characterization of BIBS 39 and BIBS 222: Two new nonpeptide angiotensin II receptor antagonists. Eur. J. Pharmacol. 218(1), 35-41 (1992).

    2. Zhang, J., Van Meel, J.C., and Van Zwieten, P.A. Antihypertensive activity of the novel, nonpeptide angiotensin II receptor antagonists BIBS 39 and BIBS 222 in conscious renal hypertensive rats. Pharmacology 46(5), 241-247 (1993).