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GSK-961081

Cat. No. M5239
GSK-961081 Structure
Synonym:

Batefenterol; TD-5959

Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 210 In stock
50mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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). 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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 740.25
Formula C40H42ClN5O7
CAS Number 743461-65-6
Purity >99%
Solubility 10mM in DMSO
Storage at -20°C
References

Pharmacologic characterization of GSK-961081 (TD-5959), a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and β2-adrenoceptor agonist properties.
Hegde SS, et al. J Pharmacol Exp Ther. 2014 Oct;351(1):190-9. PMID: 25100753.

Dual-pharmacology muscarinic antagonist and β₂ agonist molecules for the treatment of chronic obstructive pulmonary disease.
Hughes AD, et al. Future Med Chem. 2011 Oct;3(13):1585-605. PMID: 21942250.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK-961081, Batefenterol; TD-5959 supplier, Adrenergic Receptor, inhibitors

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