Terbutaline Sulfate

Alias: KWD 2019; Terbutaline sulfate; Bronclyn; Brethine; KWD-2019; KWD2019; Bricanyl; Brethaire; Terbulin
Cat No.:V1123 Purity: ≥98%
Terbutaline Sulfate (Terbutaline hemisulfate; Bronclyn, Brethine, KWD-2019; KWD2019; Bricanyl, Brethaire, Terbulin) is a potent and selective β2-adrenergic receptor agonist used for the treatment of allergic asthma.
Terbutaline Sulfate Chemical Structure CAS No.: 23031-32-5
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1g
2g
5g
10g
25g
Other Sizes

Other Forms of Terbutaline Sulfate:

  • Terbutaline
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Terbutaline Sulfate (Terbutaline hemisulfate; Bronclyn, Brethine, KWD-2019; KWD2019; Bricanyl, Brethaire, Terbulin) is a potent and selective β2-adrenergic receptor agonist used for the treatment of allergic asthma. IIt has an IC50 of 53 NM for β2-adrenergic receptor activation, while it has negligible or no effect on alpha-adrenergic receptors. The medication preferentially affects β2-adrenergic receptors, but it stimulates beta-adrenergic receptors less selectively than beta2-agonists, which are more selectively stimulating. The clinical efficacy of terbutaline in the treatment of allergic asthma is attributed to its inhibition of antigen-induced histamine release from human lung tissue that has been passively sensitized.

Biological Activity I Assay Protocols (From Reference)
Targets
β adrenergic receptor ( IC50 = 53 nM )
ln Vitro

In vitro activity: Terbutaline is an alpha-adrenergic receptor-selective β2-adrenergic bronchodilator with negligible or no effect on both. Beta-adrenergic receptors are stimulated less selectively by the drug than by relatively selective beta2-agonists, but it has a preferential effect on β2-adrenergic receptors. When used to treat allergic asthma, terbutaline is clinically effective because it blocks the release of histamine from human lung tissue that has been passively sensitized to an antigen.[1] Additionally, for all BChE variants, terbutaline exhibits competitive reversible inhibition. UU, FF, and AA homozygotes have dissociation constants of 0.18, 0.31, and 3.3 mM, in that order.[2]

ln Vivo
Terbutaline seems to stimulate beta-receptors in the uterine smooth muscles, bronchi, and vessels more strongly (β2 receptors) than it does the beta-receptors in the heart (β1 receptors). This medication may have some cardiostimulatory effects and stimulate the central nervous system in addition to relaxing smooth muscle and inhibiting uterine contractions.[3]
Cell Assay
Cell Line: J774 macrophages
Concentration: 0-10 μM
Incubation Time: 1 hour
Result: Enhanced MKP-1 expression in J774 macrophages in a dose-dependent manner.
Animal Protocol
Adult male ob/ob mice
0.5 mg/kg
Intraperitoneal injection; 0.5 mg/kg; twice a day; 20 days
References

[1]. Allergy . 1984 Jul;39(5):351-7.

[2]. J Enzyme Inhib Med Chem . 2004 Apr;19(2):113-7.

[3]. Signaling Through Hepatocyte Vasopressin Receptor 1 Protects Mouse Liver From Ischemia-Reperfusion Injury. Oncotarget. 2016 Oct 25;7(43):69276-69290.

[4]. Int J Clin Pharmacol Ther Toxicol . 1992 Sep;30(9):342-62.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H20NO5S0.5
Molecular Weight
548.65
Elemental Analysis
C, 52.54; H, 7.35; N, 5.11; O, 29.16; S, 5.84
CAS #
23031-32-5
Related CAS #
Terbutaline; 23031-25-6
Appearance
White to off-white crystalline powder
SMILES
OC1=CC(C(O)CNC(C)(C)C)=CC(O)=C1.OC2=CC(C(O)CNC(C)(C)C)=CC(O)=C2.O=S(O)(O)=O
InChi Key
KFVSLSTULZVNPG-UHFFFAOYSA-N
InChi Code
InChI=1S/2C12H19NO3.H2O4S/c2*1-12(2,3)13-7-11(16)8-4-9(14)6-10(15)5-8;1-5(2,3)4/h2*4-6,11,13-16H,7H2,1-3H3;(H2,1,2,3,4)
Chemical Name
5-(2-(tert-butylamino)-1-hydroxyethyl)benzene-1,3-diol; sulfate (2:1)
Synonyms
KWD 2019; Terbutaline sulfate; Bronclyn; Brethine; KWD-2019; KWD2019; Bricanyl; Brethaire; Terbulin
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: ~100 mg/mL (~182.3 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 0.5 mg/mL (1.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 0.5 mg/mL (1.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 120 mg/mL (437.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8227 mL 9.1133 mL 18.2266 mL
5 mM 0.3645 mL 1.8227 mL 3.6453 mL
10 mM 0.1823 mL 0.9113 mL 1.8227 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04973345 Recruiting Drug: Terbutaline Asthma Kanecia Obie Zimmerman July 7, 2023 Phase 2
Phase 3
NCT05494307 Not yet recruiting Drug: Terbutaline
Drug: Danazol
Immune Thrombocytopenia Peking University People's
Hospital
September 1, 2022 Phase 2
NCT00185887 Completed Drug: Terbutaline Fetal Distress Stanford University October 2003 Not Applicable
NCT05326269 Completed Drug: Terbutaline Nonreassuring Fetal Status Hospital Kemaman April 23, 2017 Not Applicable
NCT01096017 Completed Drug: Terbutaline Turbuhaler®
Drug: Salbutamol pMDI
Other: pMDI placebo pMDI
Asthma AstraZeneca March 2010 Phase 3
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