Tafluprost (free acid)-d4

Tafluprost (free acid)-d4 is intended for use as an internal standard for the quantification of tafluprost (free acid) (Item No. 10005439) by GC- or LC-MS. Tafluprost (free acid) is an FP receptor agonist (Ki = 4 nM for the human receptor), a derivative of prostaglandin F2α (PGF2α; Item Nos. 16010 | 16020), and an active metabolite of the prodrug tafluprost (Item No. 10005440).1 It is formed from tafluprost by hydrolysis and is selective for the FP receptor over the dopamine receptor and PGE2 receptor subtypes EP1 and EP2, as well as a panel of 32 neurological receptors and transporters, at 1 µM. Tafluprost (free acid) induces constriction in isolated cat iris sphincters (EC50 = 0.6 nM).2 It also increases the proliferation and migration of, capillary formation by, and COX-2 levels in, human umbilical vein endothelial cells (HUVECs) when used at a concentration of 100 µM.3WARNING This product is not for human or veterinary use.

[1] YASUTAKA TAKAGI . Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug[J]. Experimental eye research, 2004, 78 4: Pages 767-776. DOI: 10.1016/j.exer.2003.12.007
[2] TADASHI NAKAJIMA. New fluoroprostaglandin F(2alpha) derivatives with prostanoid FP-receptor agonistic activity as potent ocular-hypotensive agents.[J]. Biological & pharmaceutical bulletin, 2003, 26 12: 1691-1695. DOI: 10.1248/bpb.26.1691
[3] YOUNG JUNG ROH. Effects of AFP-172 on COX-2-induced angiogenic activities on human umbilical vein endothelial cells.[J]. Graefe’s Archive for Clinical and Experimental Ophthalmology, 2012, 250 12: 1765-1775. DOI: 10.1007/s00417-012-2125-2