Darapladib

SKU: orb1301065

Description

Darapladib (SB-480848) is a potent and selective Lp-PLA2 inhibitor with an IC50 of 0.25 nM. It is widely used in cardiovascular disease research to study atherosclerosis mechanisms and has demonstrated protective effects in both in vitro assays and in vivo animal models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 356057-34-6
• MW: 666.77
• Purity: 99.88%
• Formula: C₃₆H₃₈F₄N₄O₂S
• SMILES: C(C(N(CC1=CC=C(C=C1)C2=CC=C(C(F)(F)F)C=C2)CCN(CC)CC)=O)N3C4=C(C(=O)N=C3SCC5=CC=C(F)C=C5)CCC4
• Target: Apoptosis,Phospholipase
• Solubility: DMSO:123.75 mg/mL (185.6 mM);Ethanol:93 mg/mL (139.48 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Lp-PLA2:0.25 nM
• 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).
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Darapladib, Inhibitor, Lp-PLA2, inhibit, Phospholipase, SB 480848, SB480848, SB-480848

Compound Identifiers

PubChem CID

9939609