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SML1099

Roflumilast

≥98% (HPLC), powder, phosphodiesterase 4 PDE4 inhibitor

Synonym(s):

3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide, 3-Cyclopropylmethoxy-4-difluoromethoxy-N-[3,5-dichloropyrid-4-yl]-benzamide

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About This Item

Empirical Formula (Hill Notation):
C17H14Cl2F2N2O3
CAS Number:
162401-32-3
Molecular Weight:
403.21
UNSPSC Code:
41106305
PubChem Substance ID:
329825476
NACRES:
NA.77
MDL number:
MFCD00938270
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

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Product Name

Roflumilast, ≥98% (HPLC)

SMILES string

ClC1=CN=CC(Cl)=C1NC(C2=CC=C(OC(F)F)C(OCC3CC3)=C2)=O

InChI

1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24)

InChI key

MNDBXUUTURYVHR-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

−20°C

Quality Level

100

Gene Information

human ... PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144)

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This Item
SML1602SML0585SML0660
Roflumilast ≥98% (HPLC)

Sigma-Aldrich

SML1099

Roflumilast

RQ-00203078 ≥98% (HPLC)

Sigma-Aldrich

SML1602

RQ-00203078

Piclamilast ≥98% (HPLC)

Sigma-Aldrich

SML0585

Piclamilast

GSK2578215A ≥98% (HPLC)

Sigma-Aldrich

SML0660

GSK2578215A

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 25 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 15 mg/mL, clear

color

white to beige

color

white to beige

color

white to beige

color

white to beige

Application

Roflumilast has been used to evaluate its effect on acute lung inflammation and chronic lung changes in models of cigarette exposure in mice.[1] It is also used to investigate its therapeutic potential to ameliorate primary blast-induced deficits in long-term potentiation (LTP).[2]

Biochem/physiol Actions

Roflumilast is a highly potent, orally active, and selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 0.8 nM. Roflumilast has anti-inflammatory properties and is used clinically to treat COPD.
Roflumilast is a highly potent, orally active, and selective phosphodiesterase 4 (PDE4) inhibitor.

Features and Benefits

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000526513
0000526507
0000526513
0000526507
0000512436

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Fernando J Martinez et al.
Lancet (London, England), 385(9971), 857-866 (2015-02-17)
Roflumilast reduces exacerbations in patients with severe chronic obstructive pulmonary disease. Its effect in patients using fixed combinations of inhaled corticosteroids and longacting β2 agonists is unknown. We postulated that roflumilast would reduce exacerbations in patients with severe chronic obstructive
Xiaohua Du et al.
Phytotherapy research : PTR, 33(3), 602-609 (2019-01-15)
The principal active component of isoforskolin (ISOF) is from the plant Coleus forskohlii, native to China, which has attracted much attention for its biological effects. We hypothesize that ISOF and forskolin (FSK) pretreatment attenuates inflammation induced by lipopolysaccharide (LPS) related
Phosphodiesterase-4 inhibition restored hippocampal long term potentiation after primary blast.
Vogel E W, et al.
Experimental Neurology, 293, 91-100 (2017)
Christian de Mey et al.
BMC clinical pharmacology, 11, 7-7 (2011-06-03)
Roflumilast is an oral, selective phosphodiesterase 4 inhibitor with anti-inflammatory effects in chronic obstructive pulmonary disease (COPD). The addition of roflumilast to long-acting bronchodilators improves lung function in patients with moderate-to-severe COPD. The present study investigated drug-drug interaction effects between
Innocence Harvey et al.
Obesity (Silver Spring, Md.), 31(7), 1859-1870 (2023-05-31)
Prescription glucocorticoid (GC) use is widespread across developed countries for the treatment of several inflammatory conditions. Elevated GCs are known to promote lipolysis and metabolic disorders. An extract of Artemisia scoparia (SCO) has been shown to reduce lipolysis and promote
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