AS1810722
Based on 1 Customer Validation
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research.
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: 98.10%
- CAS 番号: 909561-15-5
- 分子式: C25H25F2N7O
- 分子量:477.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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STAT6 1.9 nM (IC50) |
CYP3A4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | IC50 |
2.4 nM
Compound: 24, AS1810722
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Inhibition of IL4 production in C57BL/6 mouse T cell after 16 hrs by T cell differentiation assay
Inhibition of IL4 production in C57BL/6 mouse T cell after 16 hrs by T cell differentiation assay
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[PMID: 19747833] |
? AS1810722 inhibits in vitro Th2 differentiation with an IC50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration[1].
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 mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel[1]
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Dosage:0.03-0.3 mg/kg
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Administration:Orally; 30 min before, and 24 and 48 h after OVA exposure
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Result:Suppressed eosinophil infiltration in the lung in a dose-dependent manner.
化学情報
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CAS 番号 909561-15-5
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性状 Solid
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分子量 477.51
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分子式 C25H25F2N7O
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Color Brown to black
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SMILES
O=C(N)CN1CCN(C2=CC=C(NC3=NC=C4C(N(CC5=CC(F)=CC(F)=C5)C=C4)=N3)C=C2)CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 62.5 mg/mL (130.89 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.
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.36 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 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 | 2.0942 mL | 10.4710 mL | 20.9420 mL | 52.3549 mL |
| 5 mM | 0.4188 mL | 2.0942 mL | 4.1884 mL | 10.4710 mL | |
| 10 mM | 0.2094 mL | 1.0471 mL | 2.0942 mL | 5.2355 mL | |
| 15 mM | 0.1396 mL | 0.6981 mL | 1.3961 mL | 3.4903 mL | |
| 20 mM | 0.1047 mL | 0.5235 mL | 1.0471 mL | 2.6177 mL | |
| 25 mM | 0.0838 mL | 0.4188 mL | 0.8377 mL | 2.0942 mL | |
| 30 mM | 0.0698 mL | 0.3490 mL | 0.6981 mL | 1.7452 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5235 mL | 1.3089 mL | |
| 50 mM | 0.0419 mL | 0.2094 mL | 0.4188 mL | 1.0471 mL | |
| 60 mM | 0.0349 mL | 0.1745 mL | 0.3490 mL | 0.8726 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6544 mL | |
| 100 mM | 0.0209 mL | 0.1047 mL | 0.2094 mL | 0.5235 mL |