A potent, selective β2-adrenergic receptor antagonist
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ICI 118551 (hydrochloride)

Item No. 15591

Technical Information
Formal Name
(2R,3R)-rel-1-[(2,3-dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol, monohydrochloride
CAS Number
72795-01-8
Molecular Formula
C17H27NO2 • HCl
Formula Weight
Purity
≥99%
Formulation
A crystalline solid
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 3 mg/mlEthanol: 2 mg/ml
SMILES
CC1=C(CCC2)C2=C(OC[C@H](O)[C@@H](C)NC(C)C)C=C1.Cl
InChi Code
InChI=1S/C17H27NO2.ClH/c1-11(2)18-13(4)16(19)10-20-17-9-8-12(3)14-6-5-7-15(14)17;/h8-9,11,13,16,18-19H,5-7,10H2,1-4H3;1H/t13-,16+;/m1./s1
InChi Key
KBXMBGWSOLBOQM-CACIRBSMSA-N
Shipping & Storage Information
Storage
Room temperature
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ICI 118551 is a potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively).1,2 It is active in vivo and is often used to evaluate the actions of adrenergic receptor agonists.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hoffmann, C., Leitz, M.R., Oberdorf-Maass, S., et alComparative pharmacology of human β-adrenergic receptor subtypes—characterization of stably transfected receptors in CHO cells. N.-S. Arch. Pharmacol. 369(2), 151-159 (2004).

    2. Baker, J.G. The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors. Br. J. Pharmacol. 144(3), 317-322 (2005).

    3. Deighton, N.M., Motomura, A., Bals, S., et alCharacterization of theβadrenoceptor subtype(s) mediating the positive inotropic effects of epinine, dopamine, dobutamine, denopamine and xamoterol in isolated human right atrium. J. Pharmacol. Exp. Ther. 262(2), 532-538 (1992).

    4. Rothwell, N.J., Stock, M.J., and Sudera, D.K. Changes in tissue blood flow and β-receptor density of skeletal muscle in rats treated with the β2-adrenoceptor agonist clenbuterol. Br. J. Pharmacol. 90(3), 601-607 (1987).

    5. Kim, I.M., Tilley, D.G., Chen, J., et alβ-blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation. Proc. Natl. Acad. Sci. USA 105(38), 14555-14560 (2008).