WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319652

CAS#: 743461-65-6 (free base)

Description: Batefenterol, also known as GSK961081 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.

Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same Day
25mg USD 250 Same Day
50mg USD 450 Same Day
100mg USD 750 Same Day
200mg USD 1250 Same Day
500mg USD 2350 Same Day
1g USD 3450 2 Weeks
2g USD 5450 2 Weeks
5g USD 8950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-26. Prices are subject to change without notice.

Batefenterol, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 319652
Name: Batefenterol
CAS#: 743461-65-6 (free base)
Chemical Formula: C40H42ClN5O7
Exact Mass: 739.2773
Molecular Weight: 740.254
Elemental Analysis: C, 64.90; H, 5.72; Cl, 4.79; N, 9.46; O, 15.13

Related CAS #: 945905-37-3(succinate)   743461-65-6 (free base)    

Synonym: GSK961081; GSK-961081; GSK 961081; TD-5959; TD 5959; TD5959; Batefenterol

IUPAC/Chemical Name: (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


InChi Code: InChI=1S/C40H42ClN5O7/c1-52-36-22-33(31(41)21-26(36)23-42-24-35(48)29-11-13-34(47)39-30(29)12-14-37(49)45-39)43-38(50)17-20-46-18-15-27(16-19-46)53-40(51)44-32-10-6-5-9-28(32)25-7-3-2-4-8-25/h2-14,21-22,27,35,42,47-48H,15-20,23-24H2,1H3,(H,43,50)(H,44,51)(H,45,49)/t35-/m0/s1


Technical Data

Solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Additional Information


1: Ambery CL, Wielders P, Ludwig-Sengpiel A, Chan R, Riley JH. Population Pharmacokinetics and Pharmacodynamics of GSK961081 (Batefenterol), a Muscarinic Antagonist and β2-Agonist, in Moderate-to-Severe COPD Patients: Substudy of a Randomized Trial. Drugs R D. 2015 Sep;15(3):281-91. doi: 10.1007/s40268-015-0104-x. PubMed PMID: 26286203; PubMed Central PMCID: PMC4561049.

2: Hughes AD, Chen Y, Hegde SS, Jasper JR, Jaw-Tsai S, Lee TW, McNamara A, Pulido-Rios MT, Steinfeld T, Mammen M. Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)et hyl)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 β₂ 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. Epub 2015 Feb 9. PubMed PMID: 25629394.

3: Norris V, Ambery C. Use of propranolol blockade to explore the pharmacology of GSK961081, a bi-functional bronchodilator, in healthy volunteers: results from two randomized trials. Drugs R D. 2014 Dec;14(4):241-51. doi: 10.1007/s40268-014-0060-x. PubMed PMID: 25265895; PubMed Central PMCID: PMC4269816.

4: Hegde SS, Hughes AD, Chen Y, Steinfeld T, Jasper JR, Lee TW, McNamara A, Martin WJ, Pulido-Rios MT, Mammen M. 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. Epub 2014 Aug 6. PubMed PMID: 25100753.

5: Cazzola M, Lopez-Campos JL, Puente-Maestu L. The MABA approach: a new option to improve bronchodilator therapy. Eur Respir J. 2013 Oct;42(4):885-7. doi: 10.1183/09031936.00067013. PubMed PMID: 24081753.

6: Bateman ED, Kornmann O, Ambery C, Norris V. Pharmacodynamics of GSK961081, a bi-functional molecule, in patients with COPD. Pulm Pharmacol Ther. 2013 Oct;26(5):581-7. doi: 10.1016/j.pupt.2013.03.015. Epub 2013 Mar 26. PubMed PMID: 23538170.

7: Norris V, Ambery C. Bronchodilation and safety of supratherapeutic doses of salbutamol or ipratropium bromide added to single dose GSK961081 in patients with moderate to severe COPD. Pulm Pharmacol Ther. 2013 Oct;26(5):574-80. doi: 10.1016/j.pupt.2013.03.009. Epub 2013 Mar 21. PubMed PMID: 23524017.

8: Wielders PL, Ludwig-Sengpiel A, Locantore N, Baggen S, Chan R, Riley JH. A new class of bronchodilator improves lung function in COPD: a trial with GSK961081. Eur Respir J. 2013 Oct;42(4):972-81. doi: 10.1183/09031936.00165712. Epub 2013 Feb 21. PubMed PMID: 23429913; PubMed Central PMCID: PMC3787816.

9: Cazzola M, Page C, Matera MG. Long-acting muscarinic receptor antagonists for the treatment of respiratory disease. Pulm Pharmacol Ther. 2013 Jun;26(3):307-17. doi: 10.1016/j.pupt.2012.12.006. Epub 2012 Dec 27. Review. PubMed PMID: 23274274.