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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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Anti-inflammatory agent 49 Chemical Structure

Anti-inflammatory agent 49 Chemical Structure

CAS No. : 851471-44-8

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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.

Cell Viability Assay

Cell Line: H9c2 cells[1]
Concentration: 2 µM
Incubation Time: 16 h
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].

Western Blot Analysis

Cell Line: H9c2 cells[1]
Concentration: 2 µM
Incubation Time: 24 h
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

Anti-inflammatory agent 49 (10 mg/kg, every 8 h for 72 h) rescues mice from LPS-induced endotoxemia[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c AnNCrl micee (Strain Code 028)[1]
Dosage: LPS doses 10–16.67 mg/kg, SC9 doses 10 mg/kg(after 4 h)
Administration: Intraperitoneal injection: 0.2 mL of LPS,0.1 mL of CS9; scored every 8 h for 72 h.
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.
Molecular Weight

466.52

Formula

C21H22N8O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(N(CC2=CC=CC=C2)C(N)=C1N(C)C(CSC3=NN4C(C)=CC(C)=NC4=N3)=O)=O

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1435 mL 10.7177 mL 21.4353 mL
5 mM 0.4287 mL 2.1435 mL 4.2871 mL
View the 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.

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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.

  • Protocol 1

    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.
  • Protocol 2

    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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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 2.1435 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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Anti-inflammatory agent 49
Cat. No.:
HY-155656
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