AWD 12-281
Based on 1 Customer Validation
AWD 12-281 is an orally active and highly selective phosphodiesterase 4 (PDE4) inhibitor (IC50 = 9.7 nM). AWD 12-281 is used in the study of allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis.
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 : 98.07%
- CAS 番号: 257892-33-4
- 分子式: C22H14Cl2FN3O3
- 分子量:458.27
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
生物活性
製品説明
IC50 & Target
[1]|
PDE4 9.7 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
14 nM
Compound: AWD 12-281
|
Inhibition of PDE4 isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins by liquid scintillation counting analysis
Inhibition of PDE4 isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins by liquid scintillation counting analysis
|
10.1039/C0MD00215A |
化学情報
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CAS 番号 257892-33-4
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性状 Solid
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分子量 458.27
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分子式 C22H14Cl2FN3O3
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Color Light yellow to yellow
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SMILES
O=C(C(C1=CN(CC2=CC=C(C=C2)F)C3=C1C=C(O)C=C3)=O)NC4=C(Cl)C=NC=C4Cl
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別名
GW 842470
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : 175 mg/mL (381.87 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wolfgang Bäumer, et al. AWD 12-281, a highly selective phosphodiesterase 4 inhibitor, is effective in the prevention and treatment of inflammatory reactions in a model of allergic dermatitis. J Pharm Pharmacol. 2003 Aug;55(8):1107-14. [Content Brief]
[2]. Regina Draheim, et al. Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro-pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations. J Pharmacol Exp Ther. 2004 Feb;308(2):555-63. [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 (protect from light, stored under nitrogen). 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 | 2.1821 mL | 10.9106 mL | 21.8212 mL | 54.5530 mL |
| 5 mM | 0.4364 mL | 2.1821 mL | 4.3642 mL | 10.9106 mL | |
| 10 mM | 0.2182 mL | 1.0911 mL | 2.1821 mL | 5.4553 mL | |
| 15 mM | 0.1455 mL | 0.7274 mL | 1.4547 mL | 3.6369 mL | |
| 20 mM | 0.1091 mL | 0.5455 mL | 1.0911 mL | 2.7276 mL | |
| 25 mM | 0.0873 mL | 0.4364 mL | 0.8728 mL | 2.1821 mL | |
| 30 mM | 0.0727 mL | 0.3637 mL | 0.7274 mL | 1.8184 mL | |
| 40 mM | 0.0546 mL | 0.2728 mL | 0.5455 mL | 1.3638 mL | |
| 50 mM | 0.0436 mL | 0.2182 mL | 0.4364 mL | 1.0911 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3637 mL | 0.9092 mL | |
| 80 mM | 0.0273 mL | 0.1364 mL | 0.2728 mL | 0.6819 mL | |
| 100 mM | 0.0218 mL | 0.1091 mL | 0.2182 mL | 0.5455 mL |