Cat. No.: HY-15455

Roflumilast

(Synonyms: APTA-2217; BYK 20869; B9302-107)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC₅₀s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDE4A4, PDE4B1, and PDE4B2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

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Pureté: 99.98%
CAS No.: 162401-32-3
Formule: C₁₇H₁₄Cl₂F₂N₂O₃
Masse moléculaire:403.21

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Roflumilast Chemical Structure

CAS No.: 162401-32-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

PDE4

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE) :

Cellular Effect

Cell Line	Type	Value	Description	References
Eosinophil	ED₅₀	1.8 μM/g Compound: Roflumilast	Anti-inflammatory activity against ovalbumin induced lung inflammatory rat model assessed as reduction in eosinophil influx Anti-inflammatory activity against ovalbumin induced lung inflammatory rat model assessed as reduction in eosinophil influx	[PMID: 33569941]
HEK293	IC₅₀	1 nM Compound: Roflumilast	Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay	[PMID: 20378348]
Neutrophil	ED₅₀	31 μM/g Compound: Roflumilast	Anti-inflammatory activity in LPS-induced inflammatory mouse model assessed as reduction in neutrophil influx Anti-inflammatory activity in LPS-induced inflammatory mouse model assessed as reduction in neutrophil influx	[PMID: 33569941]
PBMC	EC₅₀	50 nM Compound: Roflumilast	Anti-inflammatory activity against human PBMCs assessed as reduction in LPS-induced TNF-alpha release by ELISA analysis Anti-inflammatory activity against human PBMCs assessed as reduction in LPS-induced TNF-alpha release by ELISA analysis	[PMID: 33569941]
PBMC	IC₅₀	0.02 nM Compound: Roflumilast	Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay	[PMID: 19256507]
PBMC	IC₅₀	2.6 nM Compound: Roflumilast	Inhibition of LPS-induced TNFalpha production in PBMC Inhibition of LPS-induced TNFalpha production in PBMC	[PMID: 21871695]
Sf21	IC₅₀	>100 μM Compound: 6	Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells	[PMID: 22023548]
Sf21	IC₅₀	0.35 nM Compound: 3	Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells	[PMID: 23806553]
Sf9	IC₅₀	5.8 nM Compound: CHEMBL193240	Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate	[PMID: 26908025]
Splenocyte	IC₅₀	1.2 nM Compound: 1	Antiinflammatory activity in Balb/c mouse splenocytes assessed as LPS-induced TNF-alpha production after 18 to 24 hrs by AlphaLISA Antiinflammatory activity in Balb/c mouse splenocytes assessed as LPS-induced TNF-alpha production after 18 to 24 hrs by AlphaLISA	[PMID: 23602400]
Splenocyte	IC₅₀	1.2 nM Compound: Roflumilast	Inhibition of LPS-induced TNFalpha production in Balb/c mouse splenocytes after 18 to 24 hrs by AlphaLISA assay Inhibition of LPS-induced TNFalpha production in Balb/c mouse splenocytes after 18 to 24 hrs by AlphaLISA assay	[PMID: 24094436]

In Vitro

Roflumilast does not affect PDE enzymes apart from PDE4, and is a subnanomolar inhibitor of most PDE4 splicing variants tested. It showed no PDE4 subtype selectivity apart from PDE4C (4C1, IC₅₀=3 nM; 4C2, IC₅₀=4.3 nM), which is inhibited with a slightly lower potency^[2]. Roflumilast is a potent and selective PDE4 inhibitor. Roflumilast is a monoselective PDE4 inhibitor since it does not affect other PDE isoenzymes, including PDE1, PDE2, PDE3, and PDE5 up to 10,000-fold higher concentrations. Roflumilast inhibits human neutrophil functions. Roflumilast inhibits TNFα synthesis in monocyte-derived dendritic cells. Rolfumilast inhibits proliferation and cytokine synthesis in CD4⁺ T cells. Proliferation is inhibited to a maximum of about 60% by Roflumilast with a potency (IC₃₀) of 7 nM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Animal studies with Roflumilast demonstrated that it reduced the accumulation of neutrophils in bronchoalveolar lavage fluid following short-term exposure of guinea pigs, mice or rats to tobacco smoke, and following exposure of rats to a combination of tobacco smoke and bacterial lipopolysaccharide, and abolished the lung parenchymal influx of inflammatory cells seen in rats exposed to tobacco smoke for 7 months^[2]. Roflumilast blocks COPD progression in pIgR^/ mice. For these studies, 9-month-old WT or pIgR^/ mice are treated daily by oral gavage with 100 μg of Roflumilast (5 μg/g) or vehicle (4% methylcellulose, 1.3% PEG400) for 3 months and lungs are harvested at 12 months of age. Unlike pIgR^/ mice treated with vehicle, mice treated with Roflumilast had no progression of small airway wall remodelling after starting treatment. Strikingly, 12-month-old pIgR^/ mice treated with Roflumilast had reduced indices of emphysema compared with 9-month-old pIgR^/ mice, indicating that Roflumilast not only blocks progression of emphysema in this model but apparently facilitates some resolution of the emphysematous destruction of lung parenchyma^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 162401-32-3
Appearance Solid
Masse moléculaire 403.21
Formule C₁₇H₁₄Cl₂F₂N₂O₃
Color White to off-white
SMILES

O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC(F)F)C(OCC3CC3)=C2
Synonyms

APTA-2217; BYK 20869; B9302-107
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All Histological Imaging/Staining2D/3D Cell Culture and DifferentiationELISAWB

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Journal Impact Factor

Adv Sci (Weinh)

Dipyridamole Acts as Clinical Ferroptosis Inhibitor to Prevent from Tissue Injury. [Abstract]

2025 May 14:e2500566. PMID: 40365742
J Ethnopharmacol

Mechanism of Huanglian Zhimu Decoction in improving hepatic lipid deposition in type 2 diabetes based on lipidomics and transcriptomics. [Abstract]

2025 Jul 18;353(Pt A):120309. PMID: 40684822
J Ethnopharmacol

Chinese herbal formula Regan Saibisitan alleviates airway inflammation of chronic bronchitis via inhibiting the JAK2/STAT3 pathway. [Abstract]

2025 Jan 7:119336. PMID: 39788165

Roflumilast purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Jan 7:119336. [Abstract]

Roflumilast (ROF, 10 mg/kg, orally administered, 14 days) alleviated lung tissue pathological damage and reduced collagen deposition around the bronchi and blood vessels in CS/LPS-induced CB mice.

Roflumilast purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Jan 7:119336. [Abstract]

Roflumilast (ROF, 10 mg/kg, orally administered, 14 days) decreased IL-6, MDA, and TNF-α (p<0.0001) in the BALF of CS/LPS-induced CB mice.
Inflamm Res

Roflumilast prevents lymphotoxin α (TNF-β)-induced inflammation activation and degradation of type 2 collagen in chondrocytes. [Abstract]

2020 Dec;69(12):1191-1199. PMID: 32990777
Ceram Int

30 September 2021.
J Dermatol Sci

Roflumilast enhances the melanogenesis and attenuates oxidative stress-triggered damage in melanocytes. [Abstract]

2023 May;110(2):44-52. PMID: 37069030

Roflumilast purchased from MedChemExpress. Usage Cited in: J Dermatol Sci. 2023 May;110(2):44-52. [Abstract]

Roflumilast (10 or 100 μM), forskolin (20 or 40 μM), and the combination of 10 μM roflumilast with 20 μM forskolin exhibited no toxicity to PIG1 cells after 24 h of treatment.
Mol Cell Endocrinol

SIK1 drives lipid-induced insulin resistance in skeletal muscle by linking TGFβ1-Smad2/3 activation to PDE4-cAMP dysregulation. [Abstract]

2026 Jul:617:112788. PMID: 41856198
BMC Neurosci

Differential effects of two phosphodiesterase 4 inhibitors against lipopolysaccharide-induced neuroinflammation in mice. [Abstract]

2023 Jul 31;24(1):39. PMID: 37525115
Biochem Biophys Rep

The phosphodiesterase 4 inhibitor AA6216 suppresses activity of fibrosis-specific macrophages. [Abstract]

2021 Aug 28:28:101118. PMID: 34485715
Biochim Biophys Acta Gen Subj

Inhibition of phosphodiesterase 4 and 7 regulates breast cancer cell proliferation. [Abstract]

2025 Aug 13;1869(11):130850. PMID: 40816541
Int Urol Nephrol

The phosphodiesterase type 4 inhibitor roflumilast suppresses inflammation to improve diabetic bladder dysfunction rats. [Abstract]

2019 Feb;51(2):253-260. PMID: 30474782

Roflumilast purchased from MedChemExpress. Usage Cited in: Int Urol Nephrol. 2019 Feb;51(2):253-260. [Abstract]

Increased protein expression levels of inflammatory factors are deceased after oral Roflumilast treatment in diabetic rat DSM.
Int Urol Nephrol

Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. [Abstract]

2017 Oct;49(10):1723-1730. PMID: 28756610

Roflumilast purchased from MedChemExpress. Usage Cited in: Int Urol Nephrol. 2017 Oct;49(10):1723-1730. [Abstract]

Oral Roflumilast treatment attenuates increased expression of inflammatory factor protein in obese rat bladder. Comparison of protein expression levels of NF-κB, IL-6 in the DSM. The data are the ratio of target protein with reference. The protein levels of vehicle-treated HFDfed rats are significantly higher than those of the ND+vehicle group. The protein levels of Roflumilast-treated HFD-fed rats are significantly reduced compared to vehicle-treated HFD-fed rats. Data are shown as relative pro
Res Sq

2024 Jun 17.
Patent

US20230111925A1.

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (124.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4801 mL

12.4005 mL

24.8010 mL

5 mM

0.4960 mL

2.4801 mL

4.9602 mL

10 mM

0.2480 mL

1.2400 mL

2.4801 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.20 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocole

Kinase Assay^[3]

PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl₂, 0.5 μM cAMP or cGMP, and [³H]cAMP or [³H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[4]

Mice^[4]
WT or pIgR^−/− mice are used. For studies using Roflumilast, 200 μL of 0.5 mg/mL suspension of Roflumilast or vehicle (4% methylcellulose, 1.3% PEG400 and 5 μg drug per g animal weight) is administered by oral gavage once daily, 5 days a week for the duration of treatment. Mice are treated daily by oral gavage with 100 μg of Roflumilast (5 μg/g) or vehicle (4% methylcellulose, 1.3% PEG400) for 3 months and lungs are harvested at 12 months of age.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Hatzelmann A, et al. The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2010 Aug;23(4):235-56. [Content Brief]

[2]. Rabe KF. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67. [Content Brief]

[3]. Hatzelmann A, et al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79. [Content Brief]

[4]. Richmond BW, et al. Airway bacteria drive a progressive COPD-like phenotype in mice with polymeric immunoglobulin receptor deficiency. Nat Commun. 2016 Apr 5;7:11240. [Content Brief]

[5]. Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4801 mL	12.4005 mL	24.8010 mL	62.0024 mL
	5 mM	0.4960 mL	2.4801 mL	4.9602 mL	12.4005 mL
	10 mM	0.2480 mL	1.2400 mL	2.4801 mL	6.2002 mL
	15 mM	0.1653 mL	0.8267 mL	1.6534 mL	4.1335 mL
	20 mM	0.1240 mL	0.6200 mL	1.2400 mL	3.1001 mL
	25 mM	0.0992 mL	0.4960 mL	0.9920 mL	2.4801 mL
	30 mM	0.0827 mL	0.4133 mL	0.8267 mL	2.0667 mL
	40 mM	0.0620 mL	0.3100 mL	0.6200 mL	1.5501 mL
	50 mM	0.0496 mL	0.2480 mL	0.4960 mL	1.2400 mL
	60 mM	0.0413 mL	0.2067 mL	0.4133 mL	1.0334 mL
	80 mM	0.0310 mL	0.1550 mL	0.3100 mL	0.7750 mL
	100 mM	0.0248 mL	0.1240 mL	0.2480 mL	0.6200 mL

Keywords

Roflumilast

14 Cited Publications

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Roflumilast

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Publications Citing Use of MedChemExpress (MCE) Roflumilast

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE)

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Roflumilast Related Classifications

HY-15455 Related Classifications