tafluprost(CAS:209860-87-7)

Tafluprost (CAS 209860-87-7, code AFP-168) is a novel fluorine-modified prostaglandin small-molecule compound. Featuring ultra-high FP receptor affinity, long-acting stable intraocular pressure (IOP) lowering performance and excellent ocular safety, it has become an indispensable core research API for ophthalmic pharmacological research, glaucoma innovative drug development and generic ophthalmic formulation optimization. With the molecular formula C₂₅H₃₄F₂O₅, it maintains stable physicochemical properties with high purity and ultra-low impurities. Resistant to degradation under normal temperature and light shielding, it dissolves stably in DMSO and fully supports full-range research workflows including in vitro receptor binding assays, ocular tissue cell culture, glaucoma animal modeling, optic nerve repair experiments and high-throughput compound screening. It delivers outstanding batch uniformity and experimental repeatability, serving as the standard positive control tool compound for prostaglandin-based ophthalmic drug research.

Different from traditional IOP-lowering agents such as beta-blockers and carbonic anhydrase inhibitors that reduce aqueous humor production, Tafluprost regulates ocular pressure through a differentiated uveoscleral outflow pathway. After corneal absorption, it is hydrolyzed into biologically active metabolites that selectively activate FP receptors on ciliary muscle and trabecular meshwork tissues. It relaxes ciliary muscle, remodels extracellular matrix and unblocks aqueous drainage channels, significantly improving uveoscleral outflow efficiency and steadily reducing IOP by 20%-30% within 24 hours with durable therapeutic effects. With an ultra-low Ki value of 0.4 nM for FP receptors, its pharmacological potency is 12 times higher than Latanoprost. It exhibits exceptional target specificity with negligible activity on other prostaglandin receptor subtypes, effectively minimizing off-target side effects such as conjunctival hyperemia, iris pigmentation and eyelash hyperplasia. Once-daily administration achieves all-day IOP homeostasis with high experimental and clinical compliance, ideal for long-term chronic glaucoma intervention studies.

In scientific research applications, Tafluprost possesses multi-dimensional differentiated research value beyond single hypotensive efficacy. Firstly, it is widely applied in mechanism research of primary open-angle glaucoma and ocular hypertension, especially suitable for intractable glaucoma models intolerant to beta-blockers and multi-drug combination intervention, acting as the core reference material for evaluating the efficacy of novel IOP-lowering lead compounds. Secondly, it supports in-depth optic neuroprotection research; it inhibits retinal ganglion cell apoptosis induced by high intraocular pressure and regulates the Zn2+-mTOR pathway to promote optic nerve axon regeneration, delaying visual field defect progression in glaucoma and providing key experimental evidence for optic neurodegeneration repair. In addition, it suppresses lipid accumulation in ocular adipocytes and expands research scenarios in orbital lipid metabolism disorder and ocular surface microenvironment regulation. Its preservative-free compatibility also makes it a preferred raw material for mild high-end ophthalmic formulation development.

In terms of raw material supply and industrial research value, Tafluprost adopts mature total synthetic routes and professional fluorinated structure purification technology to efficiently remove stereoisomers and process impurities, ensuring stable and controllable biological activity across batches. Available in milligram to kilogram specifications, it fully meets the R&D demands of university basic research, CRO preclinical efficacy verification and pharmaceutical formulation development. With minimal ocular irritation, low systemic absorption, mild toxic and side effects and a wide safety experimental window, it is suitable for long-term animal model intervention. With the rising global incidence of glaucoma, long-acting, low-irritation and high-safety prostaglandin drugs have become the mainstream direction of ophthalmic innovation. Endowed with ultra-high receptor activity, comprehensive in vitro and in vivo pharmacological data and multi-functional ocular protective mechanisms, Tafluprost serves as a benchmark raw material for prostaglandin structure-activity optimization, combined medication exploration and high-end ophthalmic drug development, maintaining irreplaceable long-term core research and market value in global ophthalmic pharmacology and innovative drug R&D fields.