1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. 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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Atizoram

Atizoram Chemical Structure

CAS No. : 135637-46-6

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500 μg In-stock

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Description

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[1][2].

IC50 & Target[1]

PDE4

 

In Vitro

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.

In Vivo

Atizoram (1-32 mg/kg; p.o.; single dose) administered orally to male Balb/c mice dose-dependently elevates plasma cAMP (with a 6-fold increase at 10 mg/kg p.o.) and epinephrine, with the cAMP effect lasting up to 250 minutes, and propranolol significantly reduces the cAMP response in control mice[1].
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.

Animal Model: Balb/c (male, 20-25 g)[1]
Dosage: 1 mg/kg; 3.2 mg/kg; 10 mg/kg; 32 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Balb/c (male, 20-25 g, adrenalectomized or sham-operated)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

316.39

Formula

C18H24N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC(C=CC(C1CNC(NC1)=O)=C2)=C2O[C@@H]3[C@@H]4C[C@@H](CC4)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMF : 3 mg/mL (9.48 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1607 mL 15.8033 mL 31.6066 mL
5 mM 0.6321 mL 3.1607 mL 6.3213 mL
View the 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.

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 96.3%

References

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Atizoram
Cat. No.:
HY-108623
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