381683-94-9
381683-94-9 structure
- Name: Efipladib
- Chemical Name: Efipladib
- CAS Number: 381683-94-9
- Molecular Formula: C40H35Cl3N2O4S
- Molecular Weight: 746.14
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
- Create Date: 2017-02-03 11:19:41
- Modify Date: 2024-04-06 09:10:02
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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].
| Name | Efipladib |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
cPLA2α:0.04 μM (IC50) cPLA2α:0.067 μM (Ki) |
| In Vitro | 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: PC3 and LNCaP cells Concentration: 10, 15, 20 and 25 μM Incubation Time: 72 h Result: Significantly decreased cPLA2α activity. Increased COX-1 protein levels. Increased COX-2 protein levels in PC3 cells. |
| 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: Mouse collagen-induced arthritis (CIA) model[1] Dosage: 100 mg/kg Administration: PO, BID for 31 days Result: Gave a dramatic reduction in the clinical disease severity score relative to the vehicle treated group. Animal Model: Male Sprague-Dawley rats[2] Dosage: 100 nM in 5 μL of 100% DMSO/rat Administration: Intrathecal administration Result: Reduced PGE2 levels in the cerebrospinal fluid (CSF) by 45-60%, yet there was no effect on the nociceptive response. |
| References |
| Molecular Formula | C40H35Cl3N2O4S |
|---|---|
| Molecular Weight | 746.14 |
| Exact Mass | 744.13800 |
| PSA | 96.78000 |
| LogP | 11.24650 |