| Name | Darapladib |
| Description | Darapladib (SB-480848) is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with an IC50 value of 0.25 nM, which can exert cardiovascular protective effects [1,3]. |
| In vitro | METHODS: Bone marrow-derived macrophages (BMDM) were primed with LPS (100 ng/mL) for 3 h, then treated with 100 nM Darapladib (SB-480848) for 1 h, followed by Ang II (100 nmol/L) treatment for the indicated times.
RESULTS Darapladib (SB-480848) attenuated Ang II-induced NLRP3 inflammasome activation and IL-1β production in cardiac macrophages. [3] |
| In vivo | METHODS: Atherosclerotic Sprague-Dawley rats were fed a high-cholesterol diet for 10 weeks, followed by oral administration of low-dose Darapladib (SB-480848) (25 mg·kg-1·d-1) and high-dose Darapladib ( SB-480848) (50 mg·kg-1·d-1) intervention.
RESULTS Serum triglycerides, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), high-sensitivity C-reactive protein (hs-CRP) in the atherosclerosis model group ) and Lp-PLA2 levels were significantly increased, Rho kinase activity and cardiomyocyte apoptosis were also significantly increased (p<0.05 vs. sham operation group), while nitric oxide (NO) production was decreased; Darapladib (SB-480848 ) TC, LDL-C, CRP, Lp-PLA2, and Rho kinase activities were reduced in each group, and NO production was increased; compared with the low-dose Darapladib (SB-480848) group, TC, LDL -C, CRP, and Lp-PLA2 decreased more significantly (p<0.05), and NO production increased more significantly (p<0.05). Compared with the low-dose Darapladib (SB-480848) group, cardiomyocyte apoptosis in the high-dose Darapladib (SB-480848) group was also significantly reduced (p<0.05). However, there was no significant difference in Rho kinase activity between the low-dose Darapladib (SB-480848) group and the high-dose Darapladib (SB-480848) group (p>0.05). [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 45 mg/mL (67.49 mM)
Ethanol : 93 mg/mL (139.5 mM)
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| Keywords | SB 480848 | Phospholipase | inhibit | Inhibitor | SB480848 | Darapladib |
| Inhibitors Related | Neomycin sulfate | 1-Naphthaleneacetic acid potassium salt | trans-Benzylideneacetone | Benzylideneacetone | Tris(2,4-di-tert-butylphenyl)phosphate | (E/Z)-Polydatin | Indomethacin | Fluticasone (propionate) | 1-Naphthaleneacetic acid | Lansoprazole |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Human Metabolite Library |
United States
