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Merck
모든 사진(1)

문서

SML1099

Sigma-Aldrich

Roflumilast

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

동의어(들):

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

실험식(Hill 표기법):
C17H14Cl2F2N2O3
CAS Number:
Molecular Weight:
403.21
MDL number:
UNSPSC 코드:
41106305
PubChem Substance ID:
NACRES:
NA.77

product name

Roflumilast, ≥98% (HPLC)

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 20 mg/mL, clear

저장 온도

−20°C

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

유전자 정보

애플리케이션

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).

생화학적/생리학적 작용

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.

특징 및 장점

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.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

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

표적 기관

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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
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

문서

고리형 AMP(cAMP), 고리형 GMP(cGMP), 고리형 ADP-리보스를 포함하여 고리형 뉴클레오타이드는 GPCR 활성화에 의해 개시된 세포내 이벤트의 2차 전달자로서 광범위하게 연구되었습니다. cAMP는 주로 cAMP 의존성 단백질 인산화효소(PKA)의 활성화를 통해 모든 진핵생물 세포에서 세포 기능을 변형시키지만 cAMP 개폐 이온 채널 및 cAMP에 의해 직접 활성화되는 구아닌 뉴클레오타이드 교환 인자를 통해서도 변형시킵니다.

Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.

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