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

Name: Roflumilast
Brand: MedChemExpress
SKU: HY-15455
Rating: 5.0 (11 reviews)

Cat. No.: HY-15455 Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

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Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC₅₀s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

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

Roflumilast Chemical Structure

CAS No. : 162401-32-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 238	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Roflumilast:

9 Publications Citing Use of MCE Roflumilast

: 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.

: 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

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View All Isoforms

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PDE4

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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	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]
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: 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]
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]

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.

Clinical Trial

Molecular Weight

403.21

Formula

C₁₇H₁₄Cl₂F₂N₂O₃

CAS No.

162401-32-3

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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 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

mg/kg

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(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: 99.98%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (250 KB) HNMR (168 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Roflumilast Related Classifications

Inflammation/Immunology

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:

Roflumilast162401-32-3APTA-2217 BYK 20869 B9302-107APTA2217APTA 2217BYK20869BYK 20869BYK-20869Phosphodiesterase (PDE)RSVRespiratory syncytial virusInhibitorinhibitorinhibit

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

Customer Review

Other Forms of Roflumilast:

Roflumilast Related Antibodies

9 Publications Citing Use of MCE Roflumilast

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•Related Screening Libraries:

•Related Small Molecules:

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View All Phosphodiesterase (PDE) Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Roflumilast Related Antibodies

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Complete Stock Solution Preparation Table

Roflumilast Related Classifications

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