MRT-6160
Based on 1 Customer Validation
MRT-6160 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). MRT-6160 reduces immune cell activation, immune cell proliferation and the production of various cytokines. MRT-6160 can be used for research of inflammatory or autoimmune disorder. MRT-6160 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc..
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 3050683-38-7
- Formula: C22H17ClN2O3
- Molecular Weight:392.83
-
Storage: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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
MRT-6160 (0-1 μM, 24 h) inhibtis B cell receptor-mediated activity, specifically, MRT-6160 inhibits CD69 expression, and IL-6, lgG secretion in PBMC cells isolated from human blood leukopaks[1].
MRT-6160 (0-1 μM, 24 h) inhibits T cell receptor-mediated CD69 activation, IL-2 secretion, and proliferation of Primary T-cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MRT-6160 (1 mg/kg, p.o.) inhibits disease progression and reduces expression of calprotectin subunits (S100a8/S100a9) within colon tissue in a T cell transfer-induced model of colitis[1].
MRT-6160 (1 mg/kg, p.o.) also inhibits disease progression collagen-induced arthritis (CIA) mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 3050683-38-7
-
Appearance Solid
-
Molecular Weight 392.83
-
Formula C22H17ClN2O3
-
Color White to off-white
-
SMILES
ClC1=C(C2CCC(NC2=O)=O)C=CC=C1C3=CC=C(N4C(C=CC=C4)=O)C=C3
-
Synonyms
VAV1 degrader-3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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 (254.56 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.36 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.36 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 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Data Sheet (272 KB)
-
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)
-
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 | 2.5456 mL | 12.7282 mL | 25.4563 mL | 63.6408 mL |
| 5 mM | 0.5091 mL | 2.5456 mL | 5.0913 mL | 12.7282 mL | |
| 10 mM | 0.2546 mL | 1.2728 mL | 2.5456 mL | 6.3641 mL | |
| 15 mM | 0.1697 mL | 0.8485 mL | 1.6971 mL | 4.2427 mL | |
| 20 mM | 0.1273 mL | 0.6364 mL | 1.2728 mL | 3.1820 mL | |
| 25 mM | 0.1018 mL | 0.5091 mL | 1.0183 mL | 2.5456 mL | |
| 30 mM | 0.0849 mL | 0.4243 mL | 0.8485 mL | 2.1214 mL | |
| 40 mM | 0.0636 mL | 0.3182 mL | 0.6364 mL | 1.5910 mL | |
| 50 mM | 0.0509 mL | 0.2546 mL | 0.5091 mL | 1.2728 mL | |
| 60 mM | 0.0424 mL | 0.2121 mL | 0.4243 mL | 1.0607 mL | |
| 80 mM | 0.0318 mL | 0.1591 mL | 0.3182 mL | 0.7955 mL | |
| 100 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.6364 mL |
MRT-6160 Related Classifications
HY-168625 Related Classifications
Powered by Bioz