SML2931

GSK264220A

≥98% (HPLC)

• Synonym(s): 1-[[5-Methyl-4-[[(phenylamino)carbonyl]amino]-2-furanyl]sulfonyl]piperidine, GSK 264220A, N-[2-Methyl-5-(1-piperidinylsulfonyl)-3-furanyl]-N′-phenylurea
• Empirical Formula (Hill Notation): C₁₇H₂₁N₃O₄S
• CAS Number: 685506-42-7
• Molecular Weight: 363.43
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD02679009
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 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)
• InChI key: LVOVQRPAMXCXTM-UHFFFAOYSA-N

Description

Biochem/physiol Actions

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.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H315,H319
• pcodes: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2
• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable