SCH 351591
Based on 1 Customer Validation
SCH 351591 is a highly selective, orally active PDE4 inhibitor, with IC50 values of 58 nM and 153 nM in humans and rats, respectively. SCH 351591 effectively inhibits pathological processes such as cytokine production, eosinophilia, airway hyperresponsiveness and bronchospasm. SCH 351591 also induces microvascular injury, activates mast cells and endothelial cells, and causes increases in serum histamine and various inflammatory factors, leading to early vascular damage. SCH 351591 has been widely used in studies related to asthma, chronic obstructive pulmonary disease and drug-induced vascular injury.
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- Pureza: 99.65%
- No. CAS: 444659-43-2
- Fòrmula: C17H10Cl2F3N3O3
- Peso molecular:432.18
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
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HPDE4 58 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| U-937 | IC50 |
0.06 μM
Compound: 3a (SCH-351591)
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Inhibition of Phosphodiesterase 4 from human U937 cells
Inhibition of Phosphodiesterase 4 from human U937 cells
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[PMID: 12039576] |
SCH 351591 inhibits high-affinity rolipram (HY-16900) binding to rat brain membrane proteins with an IC50 of 153 nM (1 h)[1].
SCH 351591 (18 h) inhibits LPS-induced TNF-α production in human PBMCs with an IC50 of 59 nM[1].
SCH 351591 (48 h) inhibits stimulated IL-5 production in human peripheral blood leukocytes with an IC50 of 50 nM[1].
SCH 351591 (Multiple concentrations; 18 h) inhibits Pansorbin-induced IL-12 production in human PBMCs with an IC50 of 14 nM[1].
SCH 351591 (1 μM; 30 min) significantly inhibits anti-IgE-induced contraction of passively sensitized isolated human bronchus strips[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SCH 351591 (0.3-3 mg/kg; p.o.; single dose) inhibits LPS-induced lung neutrophilia in rats by 60% at an oral dose of 3 mg/kg[1].
SCH 351591 (3 mg/kg; p.o.; single dose) inhibits Ascaris suum-induced pulmonary inflammation in allergic cynomolgus monkeys by 79% for eosinophils, 91% for neutrophils, and 77% for total cells, without affecting acute bronchospasm[1].
SCH 351591 (5-15 mg/kg; p.o.; single dose) has a maximal nonemetic oral dose of 5 mg/kg in ferrets, with no emetic episodes observed at this dose despite substantial plasma exposure[1].
SCH 351591 (20 mg/kg; p.o.; single dose) induces a three-phase drug-induced vascular injury response starting as early as 15 minutes post-dosing in Sprague Dawley rats, with early mast cell activation, sustained serum nitrite elevation, and late increases in serum GRO/CINC-1 and granulocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BDF1 mice with Cytokine dysregulation[1]
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Dosage:2 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited serum TNF-α production by 41% at 2 mg/kg.
Increased IL-10 production from 8 ng/mL to 12 ng/mL at 2 mg/kg.
Inhibited TNF-α, IL-12 production by 77% and 47%, at 10 mg/kg.
Increased IL-10 production to 14 ng/mL at 10 mg/kg.
Inhibited TNF-α and IL-12 production by 79% and 56% at 20 mg/kg.
Increased IL-10 production to 19 ng/mL at 20 mg/kg.
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Animal Model:Sprague-Dawley rats with Pulmonary inflammation (male, 250-300 g)[1]
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Dosage:0.3 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited LPS-induced lung neutrophil influx by 60% at 3 mg/kg.
Showed no significant inhibition of lung neutrophil influx at 0.3 mg/kg.
Chemical Information
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No. CAS 444659-43-2
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Appearance Solid
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Peso molecular 432.18
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Fòrmula C17H10Cl2F3N3O3
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Color White to off-white
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SMILES
O=C(C1=C2C=CC(C(F)(F)F)=NC2=C(OC)C=C1)NC3=C(Cl)C=[N+]([O-])C=C3Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (231.39 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (281 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Billah MM, et al. Pharmacology of N-(3,5-dichloro-1-oxido-4-pyridinyl)-8-methoxy-2-(trifluoromethyl)-5-quinoline carboxamide (SCH 351591), a novel, orally active phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther. 2002;302(1):127-137. [Content Brief]
[2]. Weaver JL, et al. Early events in vascular injury in the rat induced by the phosphodiesterase IV inhibitor SCH 351591. Toxicol Pathol. 2010;38(5):738-744. [Content Brief]
[3]. Weaver JL, et al. Biomarkers in peripheral blood associated with vascular injury in Sprague-Dawley rats treated with the phosphodiesterase IV inhibitors SCH 351591 or SCH 534385. Toxicol Pathol. 2008;36(6):840-849. [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. 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 | 2.3139 mL | 11.5693 mL | 23.1385 mL | 57.8463 mL |
| 5 mM | 0.4628 mL | 2.3139 mL | 4.6277 mL | 11.5693 mL | |
| 10 mM | 0.2314 mL | 1.1569 mL | 2.3139 mL | 5.7846 mL | |
| 15 mM | 0.1543 mL | 0.7713 mL | 1.5426 mL | 3.8564 mL | |
| 20 mM | 0.1157 mL | 0.5785 mL | 1.1569 mL | 2.8923 mL | |
| 25 mM | 0.0926 mL | 0.4628 mL | 0.9255 mL | 2.3139 mL | |
| 30 mM | 0.0771 mL | 0.3856 mL | 0.7713 mL | 1.9282 mL | |
| 40 mM | 0.0578 mL | 0.2892 mL | 0.5785 mL | 1.4462 mL | |
| 50 mM | 0.0463 mL | 0.2314 mL | 0.4628 mL | 1.1569 mL | |
| 60 mM | 0.0386 mL | 0.1928 mL | 0.3856 mL | 0.9641 mL | |
| 80 mM | 0.0289 mL | 0.1446 mL | 0.2892 mL | 0.7231 mL | |
| 100 mM | 0.0231 mL | 0.1157 mL | 0.2314 mL | 0.5785 mL |
SCH 351591 Related Classifications
HY-19393 Related Classifications
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