BMS-566394
Based on 1 Customer Validation
BMS-566394 is a selective, orally active TACE (ADAM17) inhibitor. BMS-566394 inhibits LPS-induced TNF-α production in whole blood. BMS-566394 selectively inhibits TACE activity.
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- Pureté: 99.95%
- CAS No.: 503166-51-6
- Formule: C22H21F3N4O4
- Masse moléculaire:462.42
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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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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
BMS-566394 (0.3-1 μM; 5 h) inhibits LPS-induced TNF-α production in heparinized human whole blood with an IC50 of 0.130 μM, achieving 77.78% inhibition at 1 μM and 66.26% inhibition at 0.3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 503166-51-6
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Appearance Solid
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Masse moléculaire 462.42
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Formule C22H21F3N4O4
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Color White to off-white
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SMILES
O=C(N[C@H](CCOC1)[C@H]1C(NO)=O)C(C=C2)=CC=C2CN3C(C(F)(F)F)=NC4=CC=CC=C34
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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 : 100 mg/mL (216.25 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: ≥ 5 mg/mL (10.81 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.81 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
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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 (277 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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Instruction de manipulation (2659 KB)
Références
[1]. Sengupta P, et al. Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE. Eur J Med Chem. 2011;46(11):5549-5555. [Content Brief]
[2]. Moss ML, et al. Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis. Nat Clin Pract Rheumatol. 2008;4(6):300-309. [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. 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 | 2.1625 mL | 10.8127 mL | 21.6254 mL | 54.0634 mL |
| 5 mM | 0.4325 mL | 2.1625 mL | 4.3251 mL | 10.8127 mL | |
| 10 mM | 0.2163 mL | 1.0813 mL | 2.1625 mL | 5.4063 mL | |
| 15 mM | 0.1442 mL | 0.7208 mL | 1.4417 mL | 3.6042 mL | |
| 20 mM | 0.1081 mL | 0.5406 mL | 1.0813 mL | 2.7032 mL | |
| 25 mM | 0.0865 mL | 0.4325 mL | 0.8650 mL | 2.1625 mL | |
| 30 mM | 0.0721 mL | 0.3604 mL | 0.7208 mL | 1.8021 mL | |
| 40 mM | 0.0541 mL | 0.2703 mL | 0.5406 mL | 1.3516 mL | |
| 50 mM | 0.0433 mL | 0.2163 mL | 0.4325 mL | 1.0813 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3604 mL | 0.9011 mL | |
| 80 mM | 0.0270 mL | 0.1352 mL | 0.2703 mL | 0.6758 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2163 mL | 0.5406 mL |
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