A long-acting β2-adrenergic receptor agonist (EC50 = 8.71 nM for increasing intracellular cAMP levels in vitro); selective for β2-ARs over β1- and β3-ARs (Kis = 43.6

Indacaterol – 500 mg

Brand:
Cayman
CAS:
312753-06-3
Storage:
-20
UN-No:
Non-Hazardous - /

Indacaterol is a long-acting and selective β2-adrenergic receptor (β2-AR) agonist (EC50 = 8.71 nM for increasing intracellular cAMP levels in vitro).{32131} It is selective for β2-ARs over β1- and β3-ARs (Kis = 43.6, 616.6, and 3,311.3 nM, respectively). Indacaterol inhibits bronchoconstriction induced by serotonin (5-HT; Item No. 14332) in conscious guinea pigs with a maximal effect of 85% when administered intratracheally at a dose of 6.7 µg/kg. It also inhibits bronchoconstriction induced by methacholine (Item No. 23092) in rhesus monkeys with a maximal effect of 75% when administered via nebulization at a dose of 12.5 mg/kg. Formulations containing indacaterol have been used alone, and in combination with glycopyrrolate, in the treatment of chronic obstructive pulmonary disease.  

 

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Description

A long-acting β2-adrenergic receptor agonist (EC50 = 8.71 nM for increasing intracellular cAMP levels in vitro); selective for β2-ARs over β1- and β3-ARs (Kis = 43.6, 616.6, and 3,311.3 nM, respectively); inhibits 5-HT-induced bronchoconstriction in conscious guinea pigs with a maximal effect of 85% at 6.7 µg/kg intratracheally; inhibits methacholine-induced bronchoconstriction in rhesus monkeys with a maximal effect of 75% at 12.5 mg/kg via nebulization

Formal name: 5-[(1R )-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy 2(1H )-quinolinone

Synonyms:  QAB149

Molecular weight: 392.5

CAS: 312753-06-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Pulmonary Diseases|COPD/Emphysema

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