Darapladib NEW
| Price | $44 | $64 | $97 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Darapladib | CAS No.: 356057-34-6 |
| Purity: 99.85% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| 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) |
| 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 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $0.00/5mg |
VIP6Y
|
Shaanxi Dideu Medichem Co. Ltd
|
2019-12-31 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY