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AL 8810
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AL 8810图片
CAS NO:246246-19-5
规格:98%
分子量:402.5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Antagonist of prostaglandin F2α (FP) receptor.
CAS:246246-19-5
分子式:C24H31FO4
分子量:402.5
纯度:98%
存储:Store at -20°C

Background:

AL-8810 is a novel prostaglandin F2α analog that acts as a selective antagonist of prostaglandin F2α (FP) receptor.


Prostaglandin receptors are a group of g-protein coupled receptor that exhibited a variety of functions in regulation of blood pressure and renal function; smooth muscle contraction; inhibition of plate aggregation; immune response etc.


AL-8810 has a EC50 of 261 ± 44 nM against FP receptor in the A7r5 rat thoracic aorta smooth muscle cells and a EC50 of 186 ± 63 nM in Swiss mouse 3T3 fibroblasts. In addition, AL-8810 antagonizes the response to 100 nM fluprostenol (Ki = 426 ± 63 nM) in a concentration- dependent manner in A7r5 cells. [1]


In the h-TM cells, AL-8810 antagonizes the (±) fluprostenol-induced PI turn over responses concentration dependently (Ki=2.56 ± 0.62 μm). AL-8810 also antagonizes bimatoprost, travoprost acid, latanoprost acid and travoprost acid. [2] In HCM cells, 1 μm AL-8810 blocks the 85% PGF2-induced MMP-2 secretion and 66% PGF2α-induced activation of ERK1/2. [3]


参考文献:
1.  Griffin BW, Klimko P, Crider JY, Sharif NA. 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.
2.  Husain S, Jafri F, Crosson CE. Acute effects of PGF2alpha on MMP-2 secretion from human ciliary muscle cells: a PKC- and ERK-dependent process. Invest Ophthalmol Vis Sci. 2005 May;46(5):1706-13.
3.  Sharif NA, Kelly CR, Crider JY. Human trabecular meshwork cell responses induced by bimatoprost, travoprost, unoprostone, and other FP prostaglandin receptor agonist analogues. Invest Ophthalmol Vis Sci. 2003 Feb;44(2):715-21.