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Key Documents

SML1099

Sigma-Aldrich

Roflumilast

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

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C17H14Cl2F2N2O3
Numero CAS:
Peso molecolare:
403.21
Numero MDL:
Codice UNSPSC:
41106305
ID PubChem:
NACRES:
NA.77

product name

Roflumilast, ≥98% (HPLC)

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 20 mg/mL, clear

Temperatura di conservazione

−20°C

Stringa SMILE

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)
MNDBXUUTURYVHR-UHFFFAOYSA-N

Informazioni sul gene

Applicazioni

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

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Pittogrammi

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Avvertenze

Warning

Indicazioni di pericolo

Classi di pericolo

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

Organi bersaglio

Respiratory system

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (COA)

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I clienti hanno visto anche

Amparo Buenestado et al.
PloS one, 8(9), e74640-e74640 (2013-09-26)
Roflumilast is the first phosphodiesterase-4 (PDE4) inhibitor to have been approved for the treatment of COPD. The anti-inflammatory profile of PDE4 inhibitors has not yet been explored in human lung tissues. We investigated the effects of roflumilast and its active
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)
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
Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke.
Martorana P A, et al.
American Journal of Respiratory and Critical Care Medicine, 172(7), 848-853 (2005)

Contenuto correlato

Cyclic nucleotides, including cyclic AMP (cAMP), cyclic GMP (cGMP) and cyclic ADP-ribose, have been extensively studied as second messengers of intracellular events initiated by activation of GPCRs. cAMP modifies cell function in all eukaryotic cells, principally through the activation of cAMP-dependent protein kinase (PKA), but also through cAMP-gated ion channels and guanine nucleotide exchange factors directly activated by cAMP.

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