Batefenterol (GSK961081, TD-5959)

Chemical Structure : Batefenterol

CAS No.: 743461-65-6

Catalog No.: PC-43305Not For Human Use, Lab Use Only.

Batefenterol (GSK961081, TD-5959) is a bifunctional M3 mAChR antagonist and β2-adrenoceptor agonist (MABA) with pKi/pEC50 of 8.7/9.6 for hM3/hβ2 respectively, also is a small-molecule inhibitor of deubiquitinase OTUB1 with SPR KD of 23.5 uM.

Packing	Price	Stock
5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$198	In stock
50 mg	$298	In stock
100 mg		Get quote

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Biological Activity

Batefenterol (GSK961081, TD-5959) is a bifunctional M3 mAChR antagonist and β2-adrenoceptor agonist (MABA) with pKi/pEC50 of 8.7/9.6 for hM3/hβ2 respectively, also is a small-molecule inhibitor of deubiquitinase OTUB1 with SPR KD of 23.5 uM.
Batefenterol inhibits the DDX3X-DHODH axis in PC cells, significantly reduces gemcitabine resistance.
Batefenterol shows weak effect on β1.
Batefenterol is the first MABA compound to enter clinical trials and demonstrate proof of concept and efficacy in COPD.

Physicochemical Properties

M.Wt	740.2438
Formula	C40H42ClN5O7
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: 10 mM
Chemical Name/SMILES	Carbamic acid, N-[1,1'-biphenyl]-2-yl-, 1-[3-[[2-chloro-4-[[[(2R)-2-(1,2-dihydro-8-hydroxy-2-oxo-5-quinolinyl)-2-hydroxyethyl]amino]methyl]-5-methoxyphenyl]amino]-3-oxopropyl]-4-piperidinyl ester

References

1. Hughes AD, et al. J Med Chem. 2015 Mar 26;58(6):2609-22.

2. Ambery C, et al. Drugs R D. 2015 Sep;15(3):281-91.

3. Ambery C, et al. Clin Pharmacol Drug Dev. 2016 Sep;5(5):399-407.