| Bioactivity | Efipladib is a potent, selective and orally active cPLA2α inhibitor with an IC50 of 0.04 μM and a Kd of 0.067 μM[1]. |
| Invitro | Efipladib (10-25 μM; 24-72 h) 增加 PC3 和 LNCaP 细胞中 COX-1 和 PGE2 水平[3]。 Western Blot Analysis[3] Cell Line: |
| In Vivo | Efipladib (100 mg/kg; p.o.; BID for 31 days) 可逆转小鼠胶原性关节炎 (CIA) 模型的严重程度[1]。Efipladib (100 mg/kg; p.o.; once) 在给药后 1 小时显著抑制大鼠完全弗氏佐剂 (CFA) 伤害感觉模型中的伤害反应[2]。Efipladib 无法穿过血脑屏障进入中央室[2]。Efipladib (100 nM; IT; 5 μL) 降低大鼠脑脊液 PGE2 水平[2]。 Animal Model: |
| Name | Efipladib |
| CAS | 381683-94-9 |
| Formula | C40H35Cl3N2O4S |
| Molar Mass | 746.14 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. McKew J C, et al. Indole Cytosolic Phospholipase A2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3, 4-dichlorobenzyl) sulfonyl] amino} ethyl)-1-(diphenylmethyl)-1 H-indol-3-yl] propyl} benzoic Acid, Efipladib. Journal of medicinal chemistry, 2008, 51(12): 3388-3413. [2]. Nickerson-Nutter CL, et al. The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid. Neuropharmacology. 2011 Mar;60(4):633-41. [3]. Niknami M, et al. Decrease in expression or activity of cytosolic phospholipase A2alpha increases cyclooxygenase-1 action: A cross-talk between key enzymes in arachidonic acid pathway in prostate cancer cells. Biochim Biophys Acta. 2010 Jul;1801(7):731-7. |