Olodaterol

• CAT Number: R067022
• CAS Number: 868049-49-4
• Molecular Formula: C21H26N2O5
• Molecular Weight: 386.4
• Purity: ≥95%
• Storage: -20°C
• InChI: InChI=1S/C21H26N2O5/c1-21(2,10-13-4-6-15(27-3)7-5-13)22-11-18(25)16-8-14(24)9-17-20(16)28-12-19(26)23-17/h4-9,18,22,24-25H,10-12H2,1-3H3,(H,23,26)/t18-/m0/s1
• InChIKey: COUYJEVMBVSIHV-SFHVURJKSA-N
• SMILES: COC1=CC=C(CC(C)(C)N([H])C[C@H](O)C2=C(OCC(N3[H])=O)C3=CC(O)=C2)C=C1

Olodaterol is a selective agonist of β2-adrenergic receptors (β2-ARs; EC50s = 97.7 and 2,725 nM for human β2- and β1-ARs, respectively). In vivo, olodaterol completely reverses acetylcholine-induced bronchoconstriction without cardiovascular side effects in guinea pigs. It also exhibits dose-dependent bronchoprotection in a beagle model of acetylcholine-induced bronchoconstriction for a period of 24 hours, indicating potential for once-daily dosing. Formulations containing olodaterol have been used to treat bronchoconstriction associated with chronic obstructive pulmonary disease.

Reference

1.Boujyssou, T.,Hoenke, C.,Rudolf, K., et al. Discovery of olodaterol, a novel inhaled β2-adrenoceptor agonist with a 24 h bronchodilatory efficacy. Bioorg. Med. Chem. Lett. 20(4), 1410-1414 (2010).