Indacaterol maleate

SKU: orb1224070

Description

Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.

Key Properties

• CAS Number: 753498-25-8
• MW: 508.56
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₈N₂O₃
• SMILES: CCC1=C(C=C2CC(CC2=C1)NC[C@@H](C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC.C(=C\C(=O)O)\C(=O)O
• Target: Adrenergic Receptor
• Solubility: DMSO: 102 mg/mL (200.56 mM)

Bioactivity

• In Vivo:
  Animal model: Male Wistar rats (225-250 g; myocardial infarction (MI) rat model of heart failure (HF)). Dosage: 0.3 mg/kg. Administration: In animal drinking water; sinle daily for 15 weeks. Result: Significantly reduced both mean arterial blood pressure and heart rate. Increased both systolic and diastolic LVID where in HF, and reversed the decreased ejection fraction (%) values. Significantly reduced the infarct size, and catecholamine values to basal levels. Significantly increased β1 mRNA expression and cardiac cAMP levels in respect to HF.
• In Vitro:
  Cell Viability Assay Cell line: HT1080 cells (constitutively express MMP-9). Concentration: 1, 2.5, 5, 10 μM Incubation time: 12 h (pretreat). Result: Significantly suppressed MMP-9 mRNA expression in the 2.5 to 10 μM range. Cell Migration Assay Cell line: HT1080 cells (constitutively express MMP-9). Concentration: 10 μM. Incubation time: 6 h (pretreat for 2 h, then incubat with TNF-α for 4 h). Result: Significantly reduced cell migration of fibrosarcoma and inhibited HT1080 cell migration in the zone of wound healing. Western blot analysis. Cell line: HT1080 cells. Concentration: 1, 2.5, 5, 10 μM Incubation time: 2.5 h (pretreat for 2 h, then incubat with TNF-α for 0.5 h) Result: Suppressed TNF-α induced the phosphorylation of IκBα and IKKα/β (the upstream activators of NF-κB). Inhibited TNF-α-induced NF-κB nuclear translocation when at 5 and 10 μM. Suppressed TNF-α-induced MMP-9 enzyme activity and decreased MMP-9 protein levels in a dose-dependent manner in the 2.5 to 10 μM range.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Adrenergic Receptor