GS-5759
Based on 1 Customer Validation
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).
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- Purity: 99.21%
- CAS No.: 1346653-91-5
- 화학식: C47H42N6O8S
- 분자량:850.94
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보관:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
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PDE4 |
β2 adrenoceptor |
Chemical Information
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CAS No. 1346653-91-5
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Appearance Solid
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분자량 850.94
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화학식 C47H42N6O8S
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Color Light yellow to yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Joshi T, et al. GS-5759, a Bifunctional β2-Adrenoceptor Agonist and Phosphodiesterase 4 Inhibitor for Chronic Obstructive Pulmonary Disease with a Unique Mode of Action: Effects on Gene Expression in Human Airway Epithelial Cells. J Pharmacol Exp Ther. 2017 Feb;360(2):324-340. [Content Brief]
[2]. Salmon M, et al. The in vivo efficacy and side effect pharmacology of GS-5759, a novel bifunctional phosphodiesterase 4 inhibitor and long-acting β 2-adrenoceptor agonist in preclinical animal species. Pharmacol Res Perspect. 2014 Aug;2(4):e00046. [Content Brief]
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 |
GS-5759 Related Classifications
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