UNC9995
Based on 1 Customer Validation
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions.
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- Pureté: 99.93%
- CAS No.: 1354030-52-6
- Formule: C20H21Cl2N3OS
- Masse moléculaire:422.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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D2 Receptor |
UNC9995 (10 μM; 1 h) promotes the combination of STAT3 and β-arrestin2, induced by IL-6 (300 ng/mL; 24 h) in primary astrocytes. And it also inhibits activation of STING, TBK1, JAK[1].
UNC9995 (1, 5, 10, and 20 μM; 1 h) abolishes the apoptosis and inflammation of both WT and Arrb2−/− astrocytes stimulated with IL-6 (300 ng/mL) for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary astrocytes
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Concentration:10 μM
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Incubation Time:1 h for pre-incubation; with 300 ng/mL IL-6
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Result:Enhanced the interaction between STAT3 and β-arrestin2.
Abolished the activation of cGAS-STING and JAK/STAT3 pathway stimulated by IL-6, decreased the level of p-STING, p-TBK1, p-JAK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic unpredictable mild stress (CUMS) mouse model[1]
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Dosage:2 mg/kg/d
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Administration:IP; 2 weeks
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Result:Improved depressive-like symptoms of CUMS mouse model in WT mice but not Arrb2−/− mice.
Chemical Information
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CAS No. 1354030-52-6
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Appearance Solid
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Masse moléculaire 422.37
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Formule C20H21Cl2N3OS
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Color White to off-white
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SMILES
ClC1=CC=CC(N2CCN(CC2)CCCOC3=CC4=C(C=C3)SC=N4)=C1Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (118.38 mM; ultrasonic and warming and heat to 60°C; 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.
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.
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
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 | 2.3676 mL | 11.8380 mL | 23.6759 mL | 59.1898 mL |
| 5 mM | 0.4735 mL | 2.3676 mL | 4.7352 mL | 11.8380 mL | |
| 10 mM | 0.2368 mL | 1.1838 mL | 2.3676 mL | 5.9190 mL | |
| 15 mM | 0.1578 mL | 0.7892 mL | 1.5784 mL | 3.9460 mL | |
| 20 mM | 0.1184 mL | 0.5919 mL | 1.1838 mL | 2.9595 mL | |
| 25 mM | 0.0947 mL | 0.4735 mL | 0.9470 mL | 2.3676 mL | |
| 30 mM | 0.0789 mL | 0.3946 mL | 0.7892 mL | 1.9730 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5919 mL | 1.4797 mL | |
| 50 mM | 0.0474 mL | 0.2368 mL | 0.4735 mL | 1.1838 mL | |
| 60 mM | 0.0395 mL | 0.1973 mL | 0.3946 mL | 0.9865 mL | |
| 80 mM | 0.0296 mL | 0.1480 mL | 0.2959 mL | 0.7399 mL | |
| 100 mM | 0.0237 mL | 0.1184 mL | 0.2368 mL | 0.5919 mL |