Batefenterol (GSK961081, TD-5959)

Chemical Structure : Batefenterol

CAS No.: 743461-65-6

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货号: 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.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥2980	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	740.2438
分子式	C40H42ClN5O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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.