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Darapladib
产品别名
356057-34-6
Darapladib
SB-480848
SB 435445
SB 480848
SB480848
SB-435445
1-(N-(2-(Diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one
SB435445
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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C36H38F4N4O2S |
| Molecular weight | 666.77 |
| MDL number | MFCD18251452 |
| Biochem/physiol Actions【生化/生理作用】 | 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.). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| 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 |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
