Batefenterol

SKU: orb1300094

Description

Batefenterol

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 743461-65-6
• MW: 740.24
• Purity: 98.40% (May vary between batches)
• Formula: C₄₀H₄₂ClN₅O₇
• SMILES: COc1cc(NC(=O)CCN2CCC(CC2)OC(=O)Nc2ccccc2-c2ccccc2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2nc(O)ccc12
• Target: Adrenergic Receptor|||AChR
• Solubility: H2O:< 0.1 mg/mL (insoluble);DMSO:28.82 mg/mL (38.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.4 mM)

Bioactivity

• Target IC50:
  M2 (human):1.4 nM (Ki, cell free)|M3 (human):1.3 nM (Ki, cell free)|β2-adrenoceptor:3.7 nM (Ki, cell free)
• In Vivo:
  In the guinea pig broncho-protection assay, inhaled Batefenterol produces potent, dose-dependent inhibition of bronchoconstrictor responses via MA (ED50: 33.9 μg/mL), BA (ED50: 14.1 μg/mL), and MABA (ED50: 6.4 μg/mL) mechanisms. Significant bronchoprotective effects of Batefenterol are evident in guinea pigs via MA, BA, and MABA mechanisms for up to 7 days after dosing. In guinea pig isolated trachea expressing native muscarinic M3 and β2, Batefenterol produces smooth muscle relaxation through a dual mechanism involving competitive antagonism of the M3 receptor (EC50: 50 nM) and agonism of the β2 receptor (EC50: 25 nM). The combined effect on both muscarinic receptors and β2 receptors is more potent than either function working alone (EC50: 10 nM) .
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• In Vitro:
  In competition radioligand binding studies at human recombinant receptors, Batefenterol displays high affinity for hM2 (Ki; 1.4 nM), hM3 muscarinic receptors (Ki: 1.3 nM) and hβ2-adrenoceptors (Ki: 3.7 nM). Batefenterol behaves as a potent hβ2-adrenoceptor agonist (EC50: 0.29 nM for stimulation of cAMP levels) with 440- and 320-fold functional selectivity over hβ1- and hβ3-adrenoceptors, respectively .
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Storage & Handling

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

Alternative Names

β2-adrenoceptor, TD 5959, TD-5959, TD5959, AdrenergicReceptor, Adrenergic Receptor, Batefenterol, Beta Receptor, Inhibitor, GSK961081, GSK-961081, GSK 961081, mAChR, Muscarinic acetylcholine receptor, inhibit

Compound Identifiers

PubChem CID

10372836