SML2931

GSK264220A

≥98% (HPLC)

• Synonym(e): 1-[[5-Methyl-4-[[(phenylamino)carbonyl]amino]-2-furanyl]sulfonyl]piperidine, GSK 264220A, N-[2-Methyl-5-(1-piperidinylsulfonyl)-3-furanyl]-N′-phenylurea
• Empirische Formel (Hill-System): C₁₇H₂₁N₃O₄S
• CAS-Nummer: 685506-42-7
• Molekulargewicht: 363.43
• MDL-Nummer: MFCD02679009
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: [S](=O)(=O)(N3CCCCC3)c1[o]c(c(c1)NC(=O)Nc2ccccc2)C
• InChI: 1S/C17H21N3O4S/c1-13-15(19-17(21)18-14-8-4-2-5-9-14)12-16(24-13)25(22,23)20-10-6-3-7-11-20/h2,4-5,8-9,12H,3,6-7,10-11H2,1H3,(H2,18,19,21)
• InChIKey: LVOVQRPAMXCXTM-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

GSK264220A is a potent, active site-targeting, covalent inhibitor against endothelial lipase (EL or LIPG; IC₅₀ = 130 nM) and lipoprotein lipase (LPL or LIPD; IC₅₀ = 100 nM). GSK264220A reduces NeuT expression - or CoCl₂ treatment-induced intracellular triacylglycerol & lipid droplets (TAG & LD) increase in MCF-7 (16 & 32 nM) and suppresses LPL-depenent melanoma survival (by ~50% at 18.75 μM; WM852, WM1361). When applied in mice in vivo (30 mg/kg ip.), GSK264220A21 enhances lipid nanoparticles-mediated siRNAs delivery & gene-silencing efficacy.

Potent, active site-targeting, covalent inhibitor against endothelial lipase (EL, LIPG) and lipoprotein lipase (LPL, LIPD) in vitro and in vivo.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• H-Sätze: H315,H319
• P-Sätze: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• Gefahreneinstufungen: Eye Irrit. 2 - Skin Irrit. 2
• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable