| CAS NO: | 208114-93-6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 208114-93-6 |
| 化学名 | 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 |
| 分子式 | C27H37FO4 |
| 分子量 | 444.6 |
| 溶解度 | ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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