GLPG3970
Based on 1 Customer Validation
GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.70%
- No. CAS: 2403733-82-2
- Fòrmula: C25H27F3N4O4
- Peso molecular:504.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Monocyte | EC50 |
1087 nM
Compound: 3
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Induction of IL-10 expression in human CD14+ monocytes isolated from PBMC measured incubated for 1 hr followed by LPS addition further incubated for 2 hrs by ELISA assay
Induction of IL-10 expression in human CD14+ monocytes isolated from PBMC measured incubated for 1 hr followed by LPS addition further incubated for 2 hrs by ELISA assay
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[PMID: 37467565] |
| Monocyte | IC50 |
133 nM
Compound: 3
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Reduction in LPS-stimulated TNFalpha production in human CD14+ monocytes isolated from PBMC measured after 4 hrs
Reduction in LPS-stimulated TNFalpha production in human CD14+ monocytes isolated from PBMC measured after 4 hrs
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[PMID: 37467565] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2403733-82-2
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Appearance Solid
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Peso molecular 504.50
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Fòrmula C25H27F3N4O4
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Color White to off-white
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SMILES
O=C1C2=C(CCN1CC(F)(F)F)C=C(C3=CN=C4C=C(C=CN43)OCCN5CCOCC5)C=C2OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (198.22 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 1.9822 mL | 9.9108 mL | 19.8216 mL | 49.5540 mL |
| 5 mM | 0.3964 mL | 1.9822 mL | 3.9643 mL | 9.9108 mL | |
| 10 mM | 0.1982 mL | 0.9911 mL | 1.9822 mL | 4.9554 mL | |
| 15 mM | 0.1321 mL | 0.6607 mL | 1.3214 mL | 3.3036 mL | |
| 20 mM | 0.0991 mL | 0.4955 mL | 0.9911 mL | 2.4777 mL | |
| 25 mM | 0.0793 mL | 0.3964 mL | 0.7929 mL | 1.9822 mL | |
| 30 mM | 0.0661 mL | 0.3304 mL | 0.6607 mL | 1.6518 mL | |
| 40 mM | 0.0496 mL | 0.2478 mL | 0.4955 mL | 1.2389 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9911 mL | |
| 60 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8259 mL | |
| 80 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6194 mL | |
| 100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL |
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