2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. Adrenergic Receptor Phosphodiesterase (PDE)
  4. GS-5759

GS-5759 is both a β₂-adrenergic receptor agonist and a PDE4 inhibitor. GS-5759 increases intracellular cAMP levels by activating the β₂ receptor, promoting bronchial dilation. GS-5759 inhibits PDE4 activity, reduces cAMP degradation, and enhances anti-inflammatory effects. GS-5759 exhibits potent bronchial dilation and anti-inflammatory capabilities in animal models. GS-5759 can be used for research on respiratory diseases such as chronic obstructive pulmonary disease (COPD).

For research use only. We do not sell to patients.

GS-5759

GS-5759 Chemical Structure

CAS No. : 1346653-91-5

Size Price Stock Quantity
500 μg In-stock
1 mg In-stock
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

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GS-5759 Related Antibodies

Top Publications Citing Use of Products

View All Adrenergic Receptor Isoform Specific Products:

View All Isoforms
α adrenergic receptor β adrenergic receptor

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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  • Purity & Documentation

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  • Customer Review

Description

GS-5759 is both a β₂-adrenergic receptor agonist and a PDE4 inhibitor. GS-5759 increases intracellular cAMP levels by activating the β₂ receptor, promoting bronchial dilation. GS-5759 inhibits PDE4 activity, reduces cAMP degradation, and enhances anti-inflammatory effects. GS-5759 exhibits potent bronchial dilation and anti-inflammatory capabilities in animal models. GS-5759 can be used for research on respiratory diseases such as chronic obstructive pulmonary disease (COPD)[1][2].

IC50 & Target[1]

PDE4

 

β2 adrenoceptor

 

Molecular Weight

850.94

Formula

C47H42N6O8S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(NC2=CC=CC(OC)=C2)C3=CC(S(=O)(C4=CC=CC(C(NC5=CC=C(C#CCCCNC[C@@H](C6=CC=C(O)C7=C6C=CC(N7)=O)O)C=C5)=O)=C4)=O)=CC(C)=C3N=C1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (117.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1752 mL 5.8759 mL 11.7517 mL
5 mM 0.2350 mL 1.1752 mL 2.3503 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1752 mL 5.8759 mL 11.7517 mL 29.3793 mL
5 mM 0.2350 mL 1.1752 mL 2.3503 mL 5.8759 mL
10 mM 0.1175 mL 0.5876 mL 1.1752 mL 2.9379 mL
15 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9586 mL
20 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4690 mL
25 mM 0.0470 mL 0.2350 mL 0.4701 mL 1.1752 mL
30 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9793 mL
40 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
50 mM 0.0235 mL 0.1175 mL 0.2350 mL 0.5876 mL
60 mM 0.0196 mL 0.0979 mL 0.1959 mL 0.4897 mL
80 mM 0.0147 mL 0.0734 mL 0.1469 mL 0.3672 mL
100 mM 0.0118 mL 0.0588 mL 0.1175 mL 0.2938 mL
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GS-5759 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GS-57591346653-91-5GS5759GS 5759Adrenergic ReceptorPhosphodiesterase (PDE)Beta ReceptorBifunctional moleculePDE4 inhibitorLong-acting beta2-adrenoceptor agonistCOPDAnti-inflammatoryBronchodilatorForced proximityInhibitorinhibitorinhibit

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