AL-8810 

AL-8810 is a potent and selective antagonist of the PGF _2α receptor (FP receptor). AL-8810 is an activator of MAPK and ERK1/2. The K_i of the FP receptor of mouse 3T3 cells and rat A7r5 cells are 0.2±0.06 μM and 0.4±0.1 μM, respectively. AL-8810 can be used in the study of elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG)^{[1][2][3][4][5]}.

AL-8810 (0.1, 1, 10 μM, 24 h) 能明显减少 OGD 诱导损伤后的 WT 小鼠神经元细胞死亡^[2]。
AL-8810 (1, 10 μM, 24 h) 在 HEK 293 和 MG-63 细胞中通过表皮生长因子受体反激活机制促进 ERK1/2 的激活^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AL-8810 (1 或 10 mg/kg, 静脉注射) 在小鼠中减少缺血性脑损伤和神经毒性^[2]。
AL-8810 (10 mg/kg, 腹腔注射) 可改善小鼠实验性创伤性脑损伤后的预后^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

402.50

C₂₄H₃₁FO₄

246246-19-5

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Griffin BW, et al. AL-8810: a novel prostaglandin F2 alpha analog with selective antagonist effects at the prostaglandin F2 alpha (FP) receptor. J Pharmacol Exp Ther. 1999 Sep;290(3):1278-84.  [Content Brief]

  [2]. Kim YT, et al. Prostaglandin FP receptor inhibitor reduces ischemic brain damage and neurotoxicity. Neurobiol Dis. 2012 Oct;48(1):58-65. doi: 10.1016/j.nbd.2012.06.003. Epub 2012 Jun 16.  [Content Brief]

  [3]. Goupil E, et al. Biasing the prostaglandin F2α receptor responses toward EGFR-dependent transactivation of MAPK. Mol Endocrinol. 2012 Jul;26(7):1189-202.  [Content Brief]

  [4]. Sharif NA, et al. Prostaglandin FP receptor antagonists: discovery, pharmacological characterization and therapeutic utility. Br J Pharmacol. 2019 Apr;176(8):1059-1078.  [Content Brief]

  [5]. Glushakov AV, et al. Prostaglandin F2α FP receptor antagonist improves outcomes after experimental traumatic brain injury. J Neuroinflammation. 2013 Oct 30;10:132.  [Content Brief]