TD-5471 hydrochloride

SKU: orb1708398

Description

TD-5471 hydrochloride is a selective, potent, and long-acting β2-adrenergic receptor agonist developed for COPD research. It is utilized in both in vitro binding assays and in vivo models to study bronchodilation and its therapeutic potential for chronic respiratory diseases.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 530084-35-6
• MW: 558.07
• Purity: 99.57% (May vary between batches)
• Formula: C₃₂H₃₂ClN₃O₄
• SMILES: [C@@H](CNCCC1=CC=C(NC2=CC(=C(OC)C=C2)C3=CC=CC=C3)C=C1)(O)C4=C5C(=C(O)C=C4)NC(=O)C=C5.Cl
• Target: Adrenergic Receptor

Bioactivity

• Target IC50:
  guinea pig trachea:8.7 (pEC50)
• In Vivo:
  In an in vivo guinea pig model of bronchoprotection, TD-5471 demonstrates a prolonged and dose-dependent duration of action. The efficacy of TD-5471 is notably high, as evidenced by its excellent potency measured 1.5 hours after nebulized dosing. To ensure suitability for once-daily dosing in humans, a 72-hour time point is chosen, considering that a high dose of Salmeterol (300 μg/mL) provides bronchoprotection lasting ≥24 hours in this model. At the 72-hour time point, TD-5471-mediated bronchoprotection remains dose-dependent and significantly surpasses the efficacy of Salmeterol at nebulizer concentrations of ≥30 μg/mL.
• In Vitro:
  In an in vitro guinea pig trachea model, TD-5471 exhibits potent activity with a slow onset. Its potency is evident, as indicated by a pEC50 of 8.7 in the guinea pig tracheal ring assay. Notably, TD-5471 is structurally distinct from Milveterol, and its prolonged duration of action aligns with a correlation observed in other long-acting β2-agonist discovery programs, specifically related to hydrophobicity.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TD 5471 hydrochloride, TD 5471 Hydrochloride, TD5471 Hydrochloride, TD-5471 Hydrochloride, TD5471 hydrochloride, β2 adrenoceptor, β2-adrenergic receptor, Adrenergic Receptor, AdrenergicReceptor

Compound Identifiers

PubChem CID

11249914