SCH 351591

Cat. No.: HY-19393 Purity: 99.22%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

SCH 351591 Chemical Structure

CAS No. : 444659-43-2

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5 mg		Ask For Quote & Lead Time
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25 mg		Ask For Quote & Lead Time
50 mg		Ask For Quote & Lead Time
100 mg		Ask For Quote & Lead Time

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HPDE4

58 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
U-937	IC₅₀	0.06 μM Compound: 3a (SCH-351591)	Inhibition of Phosphodiesterase 4 from human U937 cells Inhibition of Phosphodiesterase 4 from human U937 cells	[PMID: 12039576]

In Vitro

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.

In Vivo

SCH 351591 (2-20 mg/kg; p.o.; single dose) dose-dependently inhibits LPS-induced TNF-α and IL-12 production and enhances IL-10 production in Corynebacterium parvum-primed mice, with significant inhibition of TNF-α at 2 mg/kg and IL-12 at 10 mg/kg^[1].
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.

Animal Model:	BDF1 mice with Cytokine dysregulation^[1]
Dosage:	2 mg/kg; 10 mg/kg; 20 mg/kg
Administration:	p.o.; single dose
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.

Animal Model:	Sprague-Dawley rats with Pulmonary inflammation (male, 250-300 g)^[1]
Dosage:	0.3 mg/kg; 3 mg/kg
Administration:	p.o.; single dose
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.

Molecular Weight

432.18

Formula

C₁₇H₁₀Cl₂F₃N₃O₃

CAS No.

444659-43-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C=CC(C(F)(F)F)=NC2=C(OC)C=C1)NC3=C(Cl)C=[N+]([O-])C=C3Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3139 mL	11.5693 mL	23.1385 mL
5 mM	0.4628 mL	2.3139 mL	4.6277 mL
10 mM	0.2314 mL	1.1569 mL	2.3139 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.22%

Select Batch:

Data Sheet (281 KB) SDS (251 KB)

COA (252 KB) HNMR (137 KB) RP-HPLC (170 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

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.

Keywords:

SCH 351591444659-43-2SCH351591SCH-351591Phosphodiesterase (PDE)type 4 phosphodiesterasehuman PBMCsasthmaPDE4guinea pig tracheal ringsU937 cellshuman peripheral blood leukocytescynomolgus monkeysSprague-Dawley ratsCorynebacterium parvum-primed miceInhibitorinhibitorinhibit

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