SML3097

Darapladib

≥98% (HPLC)

• Sinonimo/i: 1-(N-(2-(Diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one, N-[2-(Diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4′-(trifluoromethyl)[1,1′-biphenyl]-4-yl]methyl]-1H-cyclopentapyrimidine-1-acetamide, SB 435445, SB 480848, SB-435445, SB-480848, SB435445, SB480848
• Formula empirica (notazione di Hill): C₃₆H₃₈F₄N₄O₂S
• Numero CAS: 356057-34-6
• Peso molecolare: 666.77
• Numero MDL: MFCD18251452
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Forma fisica: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: O=C1N=C(SCC2=CC=C(F)C=C2)N(CC(N(CCN(CC)CC)CC3=CC=C(C4=CC=C(C(F)(F)F)C=C4)C=C3)=O)C5=C1CCC5
• InChI: 1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3; WDPFJWLDPVQCAJ-UHFFFAOYSA-N

Descrizione

Azioni biochim/fisiol

Darapladib (SB-480848) is an orally active and highly potent lipoprotein associated phospholipase A2 inhibitor (rhLp-PLA2 IC50 = 0.25 nM) with little interaction with cytochrome P450 enzymes (3A4 & 2D6 IC50 >26 μM). Darapladib effectively inhibits plasma Lp-PLA2 activtiy ex vivo (by 60% at 10 nM in human plasma & by 79% at 100 nM in Watanabe hereditable hyperlipidaemic (WHHL) rabbit plasma) and in vivo (by 95% & 91%, respectively, 3 & 5 hrs post 10 mg/kg WHHL rabbits via p.o.).

Informazioni sulla sicurezza

• 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