SML3097

Darapladib

≥98% (HPLC), phospholipase A2 inhibitor (Lp-PLA2 ), powder

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₃₆H₃₈F₄N₄O₂S
• CAS Number: 356057-34-6
• Molecular Weight: 666.77
• NACRES: NA.77
• UNSPSC Code: 12352200
• MDL number: MFCD18251452
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Product Name: Darapladib, ≥98% (HPLC)
• 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: 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
• InChI key: WDPFJWLDPVQCAJ-UHFFFAOYSA-N

Description

Biochem/physiol Actions

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.).

Orally active and highly potent lipoprotein associated phospholipase A2 inhibitor (Lp-PLA2 ) with little interaction with cytochrome P450 enzymes.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable