iST2-1
Based on 1 Customer Validation
iST2-1 is an Stimulation-2 (ST2) inhibitor with an IC50 value of 46.65 μM, blocks interaction between ST2 and IL-33, inhibits downstream signaling. iST2-1 functions as an immunomodulator, reduces proliferation of CD4+ and CD8+ T cells, increases regulatory T cell populations, reduces IFN-γ+CD4+ T cell populations, increases Foxp3+CD4+ regulatory T cell populations in the gastrointestinal tract. iST2-1 reduces plasma soluble ST2 and IFN-γ levels, reduces graft-versus-host disease scores, improves survival in graft-versus-host disease animal models, preserves graft-versus-tumor effect. iST2-1 can be used for the research of graft-versus-host disease.
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- Pureza: 99.58%
- No. CAS: 1019158-02-1
- Fòrmula: C22H22N2O4
- Peso molecular:378.42
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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ST2 46.65 μM (IC50) |
iST2-1 inhibits ST2/IL-33 binding in the AlphaLISA assay with an IC50 of 46.65 μM[1].
iST2-1 inhibits ST2/IL-33 signaling in HEK-BlueTM IL-33 cells with an IC50 range of 56.42-65.87 μM[1].
iST2-1 (1 μM) exhibits short metabolic stability in both mouse and human liver microsomes with T1/2 values of 0.73 min and 1.10 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 40 mg/kg | i.p. | 1.43 h |
iST2-1 reduces plasma sST2 concentration, decreases gastrointestinal IFNγ+CD4+ T cells, and increases gastrointestinal Foxp3+CD4+ Tregs in C3H.SW mouse GVHD models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (irradiated with 300 cGy total body irradiation, transplanted with human PBMC)[2]
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Dosage:41.4 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Reduced IFNγ+CD4+ T cells and increased Foxp3+CD4+ Tregs in gastrointestinal CD45+CD4+ cells at Day 14; Lowered plasma human IFNγ by at least 50% compared to DMSO control at Day 14; Produced more profound effects on T cell populations at Day 21; Maintained plasma hsST2 below 30 pg/mL through Day 28; Decreased GVHD score to 3; Improved survival rate to 45% on Day 35.
Chemical Information
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No. CAS 1019158-02-1
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Appearance Liquid (Density: 1.235±0.06 g/cm3)
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Peso molecular 378.42
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Fòrmula C22H22N2O4
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Color Yellow to brown
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SMILES
COC1=CC=C(C=C1)C1CCCN1CC1=CC=C(O1)C1=CC=CC=C1[N+]([O-])=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (264.26 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 (13.21 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.6426 mL | 13.2128 mL | 26.4257 mL | 66.0642 mL |
| 5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | 13.2128 mL | |
| 10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL | 6.6064 mL | |
| 15 mM | 0.1762 mL | 0.8809 mL | 1.7617 mL | 4.4043 mL | |
| 20 mM | 0.1321 mL | 0.6606 mL | 1.3213 mL | 3.3032 mL | |
| 25 mM | 0.1057 mL | 0.5285 mL | 1.0570 mL | 2.6426 mL | |
| 30 mM | 0.0881 mL | 0.4404 mL | 0.8809 mL | 2.2021 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6516 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5285 mL | 1.3213 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1011 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6606 mL |
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