AL 8810 is an 11β-fluoro analog of PGF2α which acts as a potent and selective antagonist at the FP receptor.1 AL 8810 has weak intrinsic agonist activity on FP receptor preparations in the 200-300 nM range, yet it fully antagonizes the activity of the potent FP receptor agonist fluprostenol at this concentration, with EC50 values of approximately 430 nM. AL 8810 fully antagonized the bimatoprost-induced calcium mobilization in Swiss 3T3 fibroblasts at 100 µM, indicating that bimatoprost acts as an FP agonist in this preparation.2 The Ki for the inhibition of several potent agonists at the cloned human ciliary body FP receptor is in the range of 1-2 µM.3
1Griffen, B.W., Klimko, P., Crider, J.Y., et al. AL-8810: A novel prostaglandin F2α analog with selective antagonist effects at the prostaglandin F2α (FP) receptor. J Pharmacol Exp Ther290(3)1278-1284(1999).
2Sharif, N.A., Williams, G.W., and Kelly, C.R.Bimatoprost and its free acid are prostaglandin FP receptor agonists. Eur J Pharmacol432211-213(2001).
3Sharif, N.A., Kelly, C.R., and Crider, J.Y.Agonist activity of Bimatoprost, Travoprost, Latanoprost, Unoprostone isopropyl ester and other prostaglandin analogs at the cloned human ciliary body FP prostaglandin receptor.. J Ocul Pharmacol18313-324(2002 Feb 27).
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Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.
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