Atizoram
Atizoram (CP-80,633) is an orally active phosphodiesterase type 4 (PDE4) inhibitor. Atizoram blocks cAMP degradation, thereby increasing intracellular and plasma cAMP levels. Atizoram inhibits TNFα release. Atizoram can be used in research related to acute respiratory distress syndrome.
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。
- CAS 番号: 135637-46-6
- 分子式: C18H24N2O3
- 分子量:316.39
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
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PDE4 |
Atizoram increases intracellular cAMP levels and inhibits TNFα release from monocytes in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Atizoram (1-30 mg/kg; p.o.; single dose) administered orally dose-dependently inhibits LPS-induced serum TNFα production in mice, with a slight reduction in potency after adrenalectomy (ED50 1.2 mg/kg p.o. in controls vs. 3.9 mg/kg p.o. in adx mice)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (male, 20-25 g)[1]
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Dosage:1 mg/kg; 3.2 mg/kg; 10 mg/kg; 32 mg/kg
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Administration:p.o.; single dose
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Result:Elevated plasma cAMP in a dose-dependent manner.
Elevated plasma cAMP levels as early as 10 minutes after 3.2 mg/kg p.o. dosing and remained elevated for up to 250 minutes.
Caused a 6-fold increase in plasma cAMP (from 61.1 to 360.4 pmol/mL, n=9, P<.05) at 10 mg/kg p.o. in control mice; did not significantly alter plasma cGMP levels (vehicle: 48.7 pmol/mL vs.
Atizoram: 35.7 pmol/mL, n=4, P>.05).
Caused a 2-fold increase in plasma epinephrine levels at 10 mg/kg p.o.
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Animal Model:Balb/c (male, 20-25 g, adrenalectomized or sham-operated)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently reduced LPS-induced serum TNFα production, with an ED50 of 1.2 mg/kg p.o. in control mice and an ED50 of 3.9 mg/kg p.o. in adrenalectomized mice.
Caused a greater than 95% reduction in TNFα production in control mice at 10 mg/kg p.o.
化学情報
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CAS 番号 135637-46-6
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性状 Solid
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分子量 316.39
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分子式 C18H24N2O3
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Color White to off-white
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SMILES
COC(C=CC(C1CNC(NC1)=O)=C2)=C2O[C@@H]3[C@@H]4C[C@@H](CC4)C3
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別名
CP-80,633
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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, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMF : 3 mg/mL (9.48 mM; Need ultrasonic and warming)
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). 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). 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)
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- 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]. Cheng JB, et al. The phosphodiesterase type 4 (PDE4) inhibitor CP-80,633 elevates plasma cyclic AMP levels and decreases tumor necrosis factor-alpha (TNFalpha) production in mice: effect of adrenalectomy. J Pharmacol Exp Ther. 1997;280(2):621-626. [Content Brief]
[2]. Waypa GB, et al. Oxidant-increased endothelial permeability: prevention with phosphodiesterase inhibition vs. cAMP production. J Appl Physiol (1985). 2000;88(3):835-842. [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). 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 |
|---|---|---|---|---|---|
| DMF | 1 mM | 3.1607 mL | 15.8033 mL | 31.6066 mL | 79.0164 mL |
| 5 mM | 0.6321 mL | 3.1607 mL | 6.3213 mL | 15.8033 mL |