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.
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- CAS No.: 135637-46-6
- 화학식: C18H24N2O3
- 분자량:316.39
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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.
Chemical Information
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CAS No. 135637-46-6
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Appearance Solid
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분자량 316.39
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화학식 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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Synonyms
CP-80,633
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
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| 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 |
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