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AL 8810

目录号 : GC16895

A potent, selective FP receptor antagonist

AL 8810 Chemical Structure

Cas No.:246246-19-5

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1mg
¥1,460.00
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5mg
¥6,488.00
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10mg
¥11,532.00
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25mg
¥25,205.00
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产品描述

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]

References:
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.

Chemical Properties

Cas No. 246246-19-5 SDF
化学名 (Z)-7-((1R,2R,3S,5S)-2-((R,E)-3-(2,3-dihydro-1H-inden-2-yl)-3-hydroxyprop-1-en-1-yl)-3-fluoro-5-hydroxycyclopentyl)hept-5-enoic acid
Canonical SMILES F[C@H]1C[C@H](O)[C@H](C/C=C\CCCC(O)=O)[C@H]1/C=C/[C@H](O)C2CC3=CC=CC=C3C2
分子式 C24H31FO4 分子量 402.50
溶解度 25mg/mL in DMSO, 20mg/mL in DMF 储存条件 Store at -20°C
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1 mM 2.4845 mL 12.4224 mL 24.8447 mL
5 mM 0.4969 mL 2.4845 mL 4.9689 mL
10 mM 0.2484 mL 1.2422 mL 2.4845 mL
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