ChemicalBook > CAS DataBase List > Batefenterol

Batefenterol

Product Name
Batefenterol
CAS No.
743461-65-6
Chemical Name
Batefenterol
Synonyms
Batefenterol;GSK-961081,Batefenterol;Batefenterol(GSK961081);Batefenterol, 10 mM in DMSO;GSK-961081(Batefenterol/TD-5959);GSK961081;GSK-961081;GSK 961081;TD-5959;TD 5959;TD5959;BATEFENTEROL;Batefenterol, 98%, a novel muscarinic receptor antagonist and β2-adrenoceptor agonist;GSK-961081,mAChR,inhibit,TD 5959,Muscarinic acetylcholine receptor,GSK 961081,Adrenergic Receptor,Batefenterol,Inhibitor,TD5959,Beta Receptor;(R)-1-(3-((2-Chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate;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
CBNumber
CB13145992
Molecular Formula
C40H42ClN5O7
Formula Weight
740.24
MOL File
743461-65-6.mol
More
Less

Batefenterol Property

Boiling point:
948.3±65.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:67.0(Max Conc. mg/mL);90.51(Max Conc. mM)
form 
A crystalline solid
pka
8.89±0.20(Predicted)
color 
Light yellow to yellow
More
Less

Hazard and Precautionary Statements (GHS)

More
Less

N-Bromosuccinimide Price

Cayman Chemical
Product number
21793
Product name
Batefenterol
Purity
≥98%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
21793
Product name
Batefenterol
Purity
≥98%
Packaging
5mg
Price
$202
Updated
2024/03/01
Cayman Chemical
Product number
21793
Product name
Batefenterol
Purity
≥98%
Packaging
10mg
Price
$380
Updated
2024/03/01
Cayman Chemical
Product number
21793
Product name
Batefenterol
Purity
≥98%
Packaging
25mg
Price
$830
Updated
2024/03/01
AK Scientific
Product number
7039CR
Product name
Batefenterol
Packaging
10mg
Price
$521
Updated
2021/12/16
More
Less

Batefenterol Chemical Properties,Usage,Production

Uses

Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.

in vivo

In the guinea pig bronchoprotection 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[1]. 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). Batefenterol exhibits a rapid rate of clearance and short half-life[2].

IC 50

mAChR2; mAChR3

References

[1] Hegde SS, et al. Pharmacologic characterization of GSK-961081 (TD-5959), a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and β2-adrenoceptor agonist properties. J Pharmacol Exp Ther. 2014 Oct;351(1):190-9. DOI:10.1124/jpet.114.216861
[2] Hughes AD, et al. Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist and β? agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD). J Med Chem. 2015 Mar 26;58(6):2609-22. DOI:10.1021/jm501915g

Batefenterol Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

Batefenterol Suppliers

China 69 India 1 United States 6 Global 76
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185;
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
Advantage
58
Finetech Industry Limited
Tel
027-87465837 19945049750
Fax
027-8777-2287
Email
sales@finetechnology-ind.com
Country
China
ProdList
9636
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4796
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2971
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Medi-tech Bioscientific Co., Ltd.
Tel
0519-83246372 13585352506
Fax
0519-83246372
Country
China
ProdList
1844
Advantage
58

743461-65-6, BatefenterolRelated Search:


  • GSK961081;GSK-961081;GSK 961081;TD-5959;TD 5959;TD5959;BATEFENTEROL
  • Batefenterol
  • (R)-1-(3-((2-Chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate
  • GSK-961081,Batefenterol
  • GSK-961081(Batefenterol/TD-5959)
  • Batefenterol, 98%, a novel muscarinic receptor antagonist and β2-adrenoceptor agonist
  • Batefenterol(GSK961081)
  • 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
  • GSK-961081,mAChR,inhibit,TD 5959,Muscarinic acetylcholine receptor,GSK 961081,Adrenergic Receptor,Batefenterol,Inhibitor,TD5959,Beta Receptor
  • Batefenterol, 10 mM in DMSO
  • 743461-65-6
  • C40H42ClN5O7
  • APIs