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Technical Data
| Formula | C36H38F4N4O2S |
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| Molecular Weight | 666.77 | CAS No. | 356057-34-6 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (149.97 mM) | |
| Ethanol | 100 mg/mL (149.97 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3. | ||
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| Targets |
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| In vitro | During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. [1] |
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| In vivo | In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. [1] Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. [2] In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. [3] |
Protocol (from reference)
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References
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Selleck's Darapladib has been cited by 7 publications
| The lipoprotein-associated phospholipase A2 inhibitor Darapladib sensitises cancer cells to ferroptosis by remodelling lipid metabolism [ Nat Commun, 2023, 14(1):5728] | PubMed: 37714840 |
| The lipoprotein-associated phospholipase A2 inhibitor Darapladib sensitises cancer cells to ferroptosis by remodelling lipid metabolism [ Nat Commun, 2023, 14(1):5728] | PubMed: 37714840 |
| Darapladib, an inhibitor of Lp-PLA2, sensitizes cancer cells to ferroptosis by remodeling lipid metabolism [ bioRxiv, 2023, 10.1101/2023.04.08.536136] | PubMed: None |
| Thrombin induces ACSL4-dependent ferroptosis during cerebral ischemia/reperfusion [ Signal Transduct Target Ther, 2022, 7(1):59] | PubMed: 35197442 |
| Human peroxiredoxin 6 is essential for malaria parasites and provides a host-based drug target [ Cell Rep, 2022, 39(11):110923] | PubMed: 35705035 |
| Elevated dietary ω-6 polyunsaturated fatty acids induce reversible peripheral nerve dysfunction that exacerbates comorbid pain conditions [ Nat Metab, 2021, 3(6):762-773] | PubMed: 34140694 |
| Pharmacological inhibition of eicosanoids and platelet-activating factor signaling impairs zymosan-induced release of IL-23 by dendritic cells. [Rodríguez M, et al. Biochem Pharmacol, 2016, 102:78-96] | PubMed: 26673542 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.