| CAS NO: | 208114-93-6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 444.6 |
| Cas No. | 208114-93-6 |
| Formula | C27H37FO4 |
| Solubility | ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide |
| Chemical Name | 9α,15R-dihydroxy-11β-fluoro-15-(2,3-dihydro-1H-inden-2-yl)-16,17,18,19,20-pentanor-prosta-5Z,13E-dien-1-oic acid, isopropyl ester |
| Canonical SMILES | CC(C)OC(CCC/C=C\C[C@@H]1[C@@H](/C=C/[C@H](O)C2CC3=CC=CC=C3C2)[C@@H](F)C[C@@H]1O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
EC50: 430 nM
AL 8810 is a a FP receptor antagonist.
Prostaglandin F receptor (FP), a receptor belonging to the prostaglandin (PG) group of receptors, binds to and mediates the biological actions of Prostaglandin F2α (PGF2α).
In vitro: Previous study found that AL-8810 had weak agonist potency in A7r5 cells and 3T3 fibroblasts. AL-8810 exhibited properties of an apparent competitive antagonist, which was demonstrated by producing parallel dextral shifts of the agonist concentration-response curves and no significant suppression of the maximal agonist-induced response. In addition, AL-8810 could dose-dependently antagonize the response to 100 nM fluprostenol in A7r5 cells, but however, AL-8810 could not significantly inhibit functional responses of DP, TP, EP(2), EP(4), receptor subtypes even at 10 μM concentration [1].
In vivo: In a previous study, the effect of acute intraperitoneal post-treatment with AL-8810 was studied in FP receptor knockout (FP-/-) mice after controlled cortical impact (CCI). Results showed that post-treatment with AL-8810 had no significant effect on cortical lesions, suggesting the irreversible effect of primary CCI injury, but significantly reduced hippocampal swelling. In addition, AL-8810 treatment at a dose of 10 mg/kg could significantly improve NDS after CCI, and in the AL-8810 group, CCI-induced decrease in grip strength was three-fold less [2].
Clinical trial: Up to now, AL 8810 is still in the preclinical development stage.
References:
[1] B. W. Griffen, P. Klimko, J. Y. Crider, et al. AL-8810: A novel prostaglandin F2α analog with selective antagonist effects at the prostaglandin F2α (FP) receptor. Journal of Pharmacology and Experimental Therapeutics 290(3), 1278-1284 (1999).
[2] Glushakov AV, Robbins SW, Bracy CL, Narumiya S, Doré S. Prostaglandin F2α FP receptor antagonist improves outcomes after experimental traumatic brain injury. J Neuroinflammation. 2013 Oct 30;10:132. doi: 10.1186/1742-2094-10-132.
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