All AbMole products are for research use only, cannot be used for human consumption.
GSK961081, also known as Batefenterol and TD-5959, is a Muscarinic Antagonist and β2-Agonist possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA). Batefenterol is a novel first-in-class inhaled bifunctional compound possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA). GSK-961081 displayed high affinity for hM2 (Ki = 1.4 nM), hM3 muscarinic receptors (Ki = 1.3 nM) and hβ2-adrenoceptors (Ki = 3.7 nM). GSK-961081 behaved 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.
 |
Source | J Pharmacol Exp Ther (2014). Figure 2. GSK-961081 |
| Method | Activity at Human b-Adrenoceptor Subtypes | |
| Cell Lines | BEAS-2B cells | |
| Concentrations | 10, 30, and 100 nM | |
| Incubation Time | 20 minutes | |
| Results | As shown in Table 3 and Fig. 2, GSK-961081 had an IA of 0.8, significantly greater than that of salmeterol (0.35) and albuterol (0.40), but lower than that of formoterol (0.95). |
| Cell Experiment | |
|---|---|
| Cell lines | HEK or CHO-K1 cells |
| Preparation method | Cells were incubated with increasing concentrations of GSK-961081 for 20 minutes at 37°C. The cells were stimulated with an EC90 concentration of the muscarinic agonist oxotremorine. The EC90 concentration was determined by generating an agonist concentration-response curve with the same batch of cells before the experiment. |
| Concentrations | 10, 30, and 100 nM |
| Incubation time | 20 minutes |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 740.25 |
| Formula | C40H42ClN5O7 |
| CAS Number | 743461-65-6 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Adrenergic Receptor Products |
|---|
| Indoramin
Indoramin is a selective α1A-adrenoceptor antagonist. |
| Ro 363 hydrochloride
Ro 363 hydrochloride is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is also an effective inotropic stimulant. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility. |
| Phentolamine
Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. |
| Dipivefrin
Dipivefrin is a potent adrenergic agonist. |
| HOKU-81
HOKU-81 (4-Hydroxytulobuterol) is one of the metabolites of Tulobuterol. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
