Batefenterol

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
100mg	$650	Check With Us
250mg	$1200	Check With Us
500mg	$1800	Check With Us

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Cat #: V3626 CAS #: 743461-65-6 Purity ≥ 98%

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

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	740.24
Molecular Formula	C40H42ClN5O7
CAS No.	743461-65-6
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent

Protocol	In Vitro	Batefenterol is a novel first-in-class inhaled bifunctional compound possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA). In competition radioligand binding studies at human recombinant receptors, batefenterol displays high affinity for hM2 (Ki=1.4 nM), hM3 muscarinic receptors (Ki=1.3 nM) and hβ2-adrenoceptors (Ki=3.7 nM). Batefenterol behaves 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	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

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.3509 mL	6.7546 mL	13.5091 mL	27.0183 mL
5mM	0.2702 mL	1.3509 mL	2.7018 mL	5.4037 mL
10mM	0.1351 mL	0.6755 mL	1.3509 mL	2.7018 mL
20mM	0.0675 mL	0.3377 mL	0.6755 mL	1.3509 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.