Ferroptosis-IN-22
Based on 1 Customer Validation
Ferroptosis-IN-22 is a selective ferroptosis inhibitor by targeting NCOA4 and disrupting its interaction with ferritin with an EC50 of 520 nM and a Kd of 0.78 μM. Ferroptosis-IN-22 has a strong inhibitory activity against ferroptosis induced by multiple ferroptosis inducers (RSL3 (HY-100218A), Erastin (HY-15763), ML210 (HY-100003), FIN56 (HY-103087)), but does not inhibit necrosis induced by H2O2 or apoptosis induced by STS (HY-15141). Ferroptosis-IN-22 effectively ameliorates Concanavalin A (HY-P2149)-induced acute liver injury. Ferroptosis-IN-22 can be used for the study of ferroptosis-related diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.95%
- CAS 番号: 3096878-87-1
- 分子式: C27H23NO2
- 分子量:393.48
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保管条件:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
生物活性
Ferroptosis-IN-22 (Compound 4k) exhibits anti-ferroptotic activity with EC50 values were 0.515 μM (RSL3) and 2.776 μM (Erastin) in HT-1080 cells, 0.4061 μM (RSL3) and 1.308 μM (Erastin) in 786-O cells, and 0.093 μM (RSL3) and 1.013 μM (Erastin) in MDA-MB-231 cells, and also suppresses ferroptosis induced by ML210 and FIN56[1].
Ferroptosis-IN-22 (4-8 μM) significantly reduced RSL3 or Erastin induced lipid peroxidation in both HT-1080 and 786-O cells and does not have direct antioxidative activity[1].
Ferroptosis-IN-22 (4 μM, 6 h) directly binds to NCOA4, a key receptor protein in ferritin autophagy, disrupting the interaction between NCOA4 and ferritin (FTH1), thereby inhibiting the ferritin autophagy process rather than relying on direct iron chelation in HT-1080 cells[1].
Ferroptosis-IN-22 demonstrates low cardiotoxicity and minimal risk of CYP-mediated drug-drug interactions (DDIs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080 cells
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Concentration:4 μM
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Incubation Time:6 h
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Result:Significantly reduced the amount of FTH1/FTL co-precipitated with NCOA4.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | F | Vss | Vd | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 3.751 h | 2.000 h | 557.082 ng/mL | 1474.816 ng·h/mL | 1498.461 ng·h/mL | 2.961 h | 3.263 h | 2.421 % | / | / | / |
| Rat[1] | 5 mg/kg | i.v. | 4.009 h | 0.083 h | 61139.150 ng/mL | 30464.355 ng·h/mL | 30509.903 ng·h/mL | 0.645 h | 0.689 h | / | 113.508 mL/kg | 941.525 mL/kg | 164.535 mL/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ConA induced acute liver injury model established in C57BL/6J mice[1]
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Dosage:5 and 15 mg/kg
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Administration:Intraperitoneal injection (i.p.), 24 hours and 0.5 hours before ConA injection
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Result:Decreased serum ALT and AST levels and improved liver tissue injury.
Significantly reduced the mRNA levels of TNF-α and IL-6, two major inflammatory cytokines in the liver.
Effectively reduced the levels of4-HNE and MDA, two lipid peroxidation products, in liver tissues.
Showed no effect on the morphology and the 4-HNE level of other vital organs including kidney, spleen, heart and lung.
Reduced the mRNA expression of ferroptosis marker Ptgs2.
化学情報
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CAS 番号 3096878-87-1
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性状 Solid
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分子量 393.48
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分子式 C27H23NO2
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Color White to off-white
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SMILES
CC(C)(C1=C(O)C=C2C(C(C(C3=CC=CC=C3)=C4)=C(O2)N=C4C5=CC=CC=C5)=C1)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
溶剤 & 溶解度
DMSO : 100 mg/mL (254.14 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (6.35 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 (6.35 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:
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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.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5414 mL | 12.7071 mL | 25.4143 mL | 63.5356 mL |
| 5 mM | 0.5083 mL | 2.5414 mL | 5.0829 mL | 12.7071 mL | |
| 10 mM | 0.2541 mL | 1.2707 mL | 2.5414 mL | 6.3536 mL | |
| 15 mM | 0.1694 mL | 0.8471 mL | 1.6943 mL | 4.2357 mL | |
| 20 mM | 0.1271 mL | 0.6354 mL | 1.2707 mL | 3.1768 mL | |
| 25 mM | 0.1017 mL | 0.5083 mL | 1.0166 mL | 2.5414 mL | |
| 30 mM | 0.0847 mL | 0.4236 mL | 0.8471 mL | 2.1179 mL | |
| 40 mM | 0.0635 mL | 0.3177 mL | 0.6354 mL | 1.5884 mL | |
| 50 mM | 0.0508 mL | 0.2541 mL | 0.5083 mL | 1.2707 mL | |
| 60 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0589 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3177 mL | 0.7942 mL | |
| 100 mM | 0.0254 mL | 0.1271 mL | 0.2541 mL | 0.6354 mL |