Anti-inflammatory agent 49
Based on 1 publication(s) in Google Scholar
nti-inflammatory agent 49 (compound SC9) is a quite potent and selective inhibitor of Drp1-Fis1 interaction and can reduce FIS1-mediated mitochondrial dysfunction. The IC50 of SC9 inhibiting GTPase in vitro is 270 nM.
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- Pureté : 99.44%
- CAS No.: 851471-44-8
- Formule: C21H22N8O3S
- Masse moléculaire:466.52
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Anti-inflammatory agent 49
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Activité biologique
Description
IC50 & Target
IC50: 270 nM (dynamin-related protein 1 ,Drp1 )[1]
In Vitro
1.Anti-inflammatory agent 49 can reduce the mitochondrial dysfunction of H9c2 cells induced by LPS (HY-D1056) and save the mice endotoxemia induced by LPS[1].
2.Anti-inflammatory agent 49 inhibits Drp1 association with the mitochondria and Drp1-Fis1 interaction following LPS treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:H9c2 cells[1]
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Concentration:2 µM
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Incubation Time:16 h
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Result:Decreased the percentage of cells with fragmented mitochondria. The percent of fragmented cells was decreased from 22% (LPS + Veh) to 9% (LPS + SC9), relative to 4% in the absence of LPS[1].
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Cell Line:H9c2 cells[1]
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Concentration:2 µM
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Incubation Time:24 h
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Result:Decreased the number of high Drp1-Fis1 cells from 67% (LPS + Veh) to 28% (LPS + P110) and to 14% (LPS + SC9).[1]
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c AnNCrl micee (Strain Code 028)[1]
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Dosage:LPS doses 10–16.67 mg/kg, SC9 doses 10 mg/kg(after 4 h)
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Administration:Intraperitoneal injection: 0.2 mL of LPS,0.1 mL of CS9; scored every 8 h for 72 h.
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Result:Improved mouse survival at all LPS doses tested at the different LPS doses (10 to 16.6 mg/kg) .
Dramatically reduced the occurrence of critical symptoms such as respiratory distress.
Chemical Information
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CAS No. 851471-44-8
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Appearance Solid
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Masse moléculaire 466.52
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Formule C21H22N8O3S
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Color White to off-white
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SMILES
O=C1NC(N(CC2=CC=CC=C2)C(N)=C1N(C)C(CSC3=NN4C(C)=CC(C)=NC4=N3)=O)=O
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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
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (214.35 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 (5.36 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 (5.36 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.
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.
Protocole
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
Pureté et documentation
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Fiche technique (274 KB)
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SDS (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 | 2.1435 mL | 10.7177 mL | 21.4353 mL | 53.5883 mL |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.2871 mL | 10.7177 mL | |
| 10 mM | 0.2144 mL | 1.0718 mL | 2.1435 mL | 5.3588 mL | |
| 15 mM | 0.1429 mL | 0.7145 mL | 1.4290 mL | 3.5726 mL | |
| 20 mM | 0.1072 mL | 0.5359 mL | 1.0718 mL | 2.6794 mL | |
| 25 mM | 0.0857 mL | 0.4287 mL | 0.8574 mL | 2.1435 mL | |
| 30 mM | 0.0715 mL | 0.3573 mL | 0.7145 mL | 1.7863 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5359 mL | 1.3397 mL | |
| 50 mM | 0.0429 mL | 0.2144 mL | 0.4287 mL | 1.0718 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3573 mL | 0.8931 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2679 mL | 0.6699 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5359 mL |
Anti-inflammatory agent 49 Related Classifications
HY-155656 Related Classifications
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