Suprofen - Moligand™, 10mM in DMSO , Cyclooxygenase inhibitor, CAS No.40828-46-4, Cyclooxygenase inhibitor

CAS: 40828-46-4 Cat. No.: S408492 Peso molecular: 260.31 Número EC: 255-096-9 PubChem CID: 5359

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

α-​methyl-​4-​(2-​thienylcarbonyl)​-benzeneacetic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Suprofen is a dualCOX-1/COX-2inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
In vitro

Suprofen inactivates the diclofenac-4-hydroxylase activity of baculovirus-expressed P450 2C9 in a time- and concentration-dependent manner, which is consistent with mechanism-based inactivation. Suprofen is a known generator of singlet oxygen whose participation in the reaction is supported by the effects of quenchers and scavengers. Suprofen photosensitizes the production of alkali-labile cleavage sites in DNA much more efficiently than direct strand breaks. Suprofen sensitizes photo-oxidation of cholesterol, producing 7 alpha- and 7 beta-hydroperoxides but not 5 alpha-hydroperoxide of cholesterol. Suprofen-sensitized photo-oxidation of membrane lipids of liposomes increases leakage of trapped glucose, suggesting photosensitized destabilization of the membrane structure. Suprofen incorporation in the phosphatidylcholine (PC) evaporation vesicles (REV) membrane leads to approximately 5% increase in the encapsulation efficiency (34%) in comparison to standard REV (29%).

In vivo

Suprofen combined with PGF2 alpha blocks induction of uterine contractions, suggesting the possibility that Suprofen also antagonizes PGF2 alpha receptor binding. Suprofen are effective at preventing BAB disruption after paracentesis in dogs, indicating their potential usefulness for treatment of prostaglandin-mediated ocular disease. Suprofen (3.7 mg/kg, i.v.) induces a marked decrease in the firing evoked in arthritic rats by ankle mobilization.
Cell Data

cell lines：HCC1806, MDA-MB-231, and T47D cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

α-​methyl-​4-​(2-​thienylcarbonyl)​-benzeneacetic acid

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Cyclooxygenase inhibitor

Propiedades del producto

• ALogP: 3.3

Nombres e identificadores

• Isómeros SMILES: CC(C1=CC=C(C=C1)C(=O)C2=CC=CS2)C(=O)O
• PubChem CID: 5359
• Peso molecular: 260.31

Objetivos asociados (humanos)

PTGS1 Tclin Prostaglandin G/H synthase 1 (2 Activities)

Discover Target: PTGS1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 (1 Activities)

Discover Target: PTGS2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro Water: 42 mg/mL (200.35 mM); DMSO: Insoluble; Ethanol: Insoluble
• Punto de fusión (°C): 123 °C

Referencias

1. Yuanjing Lin, Jialiang Guo, Hang Lin, Jincai Wang, Govert W. Somsen, Jacques Crommen, Zhengjin Jiang.  (2017)  Effect of fabrication strategy on the enantioseparation performance of β-cyclodextrin-functionalized polymethacrylate monoliths: A comparative evaluation.  JOURNAL OF SEPARATION SCIENCE,  40  (19): (3754-3762).  [PMID:28749038] [10.1002/jssc.201700424]

2. Jialiang Guo, Yuan Xiao, Yuanjing Lin, Jacques Crommen, Zhengjin Jiang.  (2016)  Effect of the crosslinker type on the enantioseparation performance of β-cyclodextrin functionalized monoliths prepared by the one-pot approach.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:27268520] [10.1016/j.chroma.2016.05.078]

3. Jialiang Guo, Yuan Xiao, Yuanjing Lin, Qiaoxuan Zhang, Yiqun Chang, Jacques Crommen, Zhengjin Jiang.  (2016)  Influence of the linking spacer length and type on the enantioseparation ability of β-cyclodextrin functionalized monoliths.  TALANTA,      [PMID:26992519] [10.1016/j.talanta.2016.02.016]