RIP1 kinase inhibitor 1
Based on 1 Customer Validation
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04).
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: 99.96%
- CAS 番号: 2095515-38-9
- 分子式: C24H20ClN5O3
- 分子量:461.90
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
pKi: 9.04 (RIP1 kinase)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
2 nM
Compound: 22
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Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity
Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity
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[PMID: 29485864] |
| L929 | IC50 |
15 nM
Compound: 22
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Induction of necroptosis in mouse L929 cells assessed as increase in TNFalpha/zVAD-FMK-induced LDH release preincubated for 30 mins followed by TNFalpha/zVAD-FMK addition measured after 4 hrs by CytoTox 96 nonradioactive cytotoxicity assay
Induction of necroptosis in mouse L929 cells assessed as increase in TNFalpha/zVAD-FMK-induced LDH release preincubated for 30 mins followed by TNFalpha/zVAD-FMK addition measured after 4 hrs by CytoTox 96 nonradioactive cytotoxicity assay
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[PMID: 29485864] |
RIP1 kinase inhibitor 1 (compound 22) strongly suppresses necroptotic cell death and phosphorylation of MLKL(pMLKL) in human colorectal adenocarcinoma HT-29 cells (nectoptosis, IC50=2 nM; pMLKL, IC50=1.3 nM) as well as mouse L-cells NCTC 929 (nectoptosis, IC50=15 nM; pMLKL, IC50=2.7 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2095515-38-9
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性状 Solid
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分子量 461.90
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分子式 C24H20ClN5O3
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Color White to yellow
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SMILES
N#CC1=CC=C2N(C)C([C@@H](N3CCC4=C(Cl)N(CC5=CC=CC=C5)N=C4C3=O)COC2=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 200 mg/mL (432.99 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: 5 mg/mL (10.82 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (272 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Yoshikawa M, et al. Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, OrallyAvailable, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships. J Med Chem. 2018 Mar 22;61(6):2384-2409. [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 (sealed storage, away from moisture and light). 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 | 2.1650 mL | 10.8249 mL | 21.6497 mL | 54.1243 mL |
| 5 mM | 0.4330 mL | 2.1650 mL | 4.3299 mL | 10.8249 mL | |
| 10 mM | 0.2165 mL | 1.0825 mL | 2.1650 mL | 5.4124 mL | |
| 15 mM | 0.1443 mL | 0.7217 mL | 1.4433 mL | 3.6083 mL | |
| 20 mM | 0.1082 mL | 0.5412 mL | 1.0825 mL | 2.7062 mL | |
| 25 mM | 0.0866 mL | 0.4330 mL | 0.8660 mL | 2.1650 mL | |
| 30 mM | 0.0722 mL | 0.3608 mL | 0.7217 mL | 1.8041 mL | |
| 40 mM | 0.0541 mL | 0.2706 mL | 0.5412 mL | 1.3531 mL | |
| 50 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0825 mL | |
| 60 mM | 0.0361 mL | 0.1804 mL | 0.3608 mL | 0.9021 mL | |
| 80 mM | 0.0271 mL | 0.1353 mL | 0.2706 mL | 0.6766 mL | |
| 100 mM | 0.0216 mL | 0.1082 mL | 0.2165 mL | 0.5412 mL |
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