| Bioactivity | Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM[1]. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist[2]. | |||||||||
| Target | IC50: 230 pM (Lp-PLA2). | |||||||||
| Invitro | Rilapladib through reduction of the PAF biological activity (as PAF inhibitors) and PAF levels could reduce Lp-PLA2 biosynthesis and prevent the possible adverse effects of Lp-PLA2[2]. | |||||||||
| Name | Rilapladib | |||||||||
| CAS | 412950-08-4 | |||||||||
| Formula | C40H38F5N3O3S | |||||||||
| Molar Mass | 735.81 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Shaddinger BC, et al. Platelet aggregation unchanged by lipoprotein-associated phospholipase A₂ inhibition: results from an in vitro study and two randomized phase I trials. PLoS One. 2014 Jan 27;9(1):e83094. [2]. Athanasios Papakyriakou, et al. Computational Investigation of Darapladib and Rilapladib Binding to Platelet Activating Factor Receptor. A Possible Mechanism of Their Involvement in Atherosclerosis. International Journal of Chemistry; Vol. 6, No. 1; 2014. |
Rilapladib
CAS: 412950-08-4 F: C40H38F5N3O3S W: 735.81
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM
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