ロフルミラスト (Synonyms: Roflumilast; APTA-2217; BYK 20869; B9302-107)

Name: Roflumilast
Brand: MedChemExpress
SKU: HY-15455
Rating: 5.0 (14 reviews)

製品番号: HY-15455 純度: 99.98%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 162401-32-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$66	在庫あり	Estimated Time of Arrival: December 31
10 mg	$79	在庫あり	Estimated Time of Arrival: December 31
25 mg	$158	在庫あり	Estimated Time of Arrival: December 31
50 mg	$238	在庫あり	Estimated Time of Arrival: December 31
100 mg	$360	在庫あり	Estimated Time of Arrival: December 31
500 mg	$800	在庫あり	Estimated Time of Arrival: December 31
1 g		お問い合わせ
5 g		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Other Forms of Roflumilast:

Roflumilast N-oxide 在庫あり
Roflumilast Impurity E 在庫あり
Roflumilast-d₄ 在庫あり
Roflumilast-d₄ N-Oxide 在庫あり
Roflumilast-d₃ お問い合わせ
Roflumilast (Standard) お問い合わせ

顧客検証

Histological Imaging/Staining

2D/3D Cell Culture and Differentiation

ELISA

: 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.

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

: 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

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

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

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

PDE4

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	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]
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]
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]

体外実験

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.

体内実験

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.

臨床実験

分子量

403.21

分子式

C₁₇H₁₄Cl₂F₂N₂O₃

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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.

純度とドキュメンテーション

純度: 99.98%

Select Batch:

データシート (282 KB) SDS (393 KB)

COA (250 KB) HNMR (276 KB) RP-HPLC (258 KB) MS (69 KB)

取扱説明書 (2659 KB)

参考文献

[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]

キナーゼ実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

Molarity Calculator
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The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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ロフルミラスト (Synonyms: Roflumilast; APTA-2217; BYK 20869; B9302-107)

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ロフルミラスト (Synonyms: Roflumilast; APTA-2217; BYK 20869; B9302-107)

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Other Forms of Roflumilast:

ロフルミラスト 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

ロフルミラスト 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Roflumilast Related Classifications

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Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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ロフルミラスト関連抗体

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