GP130 receptor agonist-1
Based on 1 Customer Validation
GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 339303-87-6
- Formula: C15H11FN2S
- Molecular Weight:270.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| J774.A1 | IC50 |
>100 μM
Compound: 15
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Antileishmanial activity against Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase reporter gene infected in mouse J-774A1 cells assessed as inhibition of amastigote stage formation incubated for 72 hrs by luminometry
Antileishmanial activity against Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase reporter gene infected in mouse J-774A1 cells assessed as inhibition of amastigote stage formation incubated for 72 hrs by luminometry
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[PMID: 26318065] |
In SH-SY5Y cells, GP130 receptor agonist-1 (Compound 2) treatment showed a 2-fold increase in phosphorylation of STAT3 within 10 min at its regulatory Tyr705 site. In primary hippocampal neuronal cultures, the pSTAT3 levels are below levels of detection for GP130 receptor agonist-1 at all time points[1].
GP130 receptor agonist-1 treatment shows increases phosphorylation of AKT at its regulatory Thr308 site and phosphorylation of ERK1/2 at its regulatory Thr202/Tyr204 site in the serum free media condition in SH-SY5Y cells, and in primary cortical neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 339303-87-6
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Appearance Solid
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Molecular Weight 270.32
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Formula C15H11FN2S
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Color White to off-white
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SMILES
FC1=CC=C(C=C1)NC2=NC(C3=CC=CC=C3)=CS2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (369.93 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. 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. 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 (9.25 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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. 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 | 3.6993 mL | 18.4966 mL | 36.9932 mL | 92.4830 mL |
| 5 mM | 0.7399 mL | 3.6993 mL | 7.3986 mL | 18.4966 mL | |
| 10 mM | 0.3699 mL | 1.8497 mL | 3.6993 mL | 9.2483 mL | |
| 15 mM | 0.2466 mL | 1.2331 mL | 2.4662 mL | 6.1655 mL | |
| 20 mM | 0.1850 mL | 0.9248 mL | 1.8497 mL | 4.6241 mL | |
| 25 mM | 0.1480 mL | 0.7399 mL | 1.4797 mL | 3.6993 mL | |
| 30 mM | 0.1233 mL | 0.6166 mL | 1.2331 mL | 3.0828 mL | |
| 40 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3121 mL | |
| 50 mM | 0.0740 mL | 0.3699 mL | 0.7399 mL | 1.8497 mL | |
| 60 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5414 mL | |
| 80 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 100 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL |