Reproxzlap(CAS:916056-79-6)

Reproxalap, development code ADX-102, CAS 916056-79-6, is a first-in-class covalent reactive aldehyde species (RASP) small-molecule inhibitor originally developed by Aldeyra Therapeutics in the United States. With an innovative aldehyde-scavenging anti-inflammatory mechanism, it breaks the technical limitations of traditional ophthalmic anti-inflammatory drugs that rely on hormone therapy or cytokine antagonism, establishing itself as a benchmark core research API for dry eye disease pharmacology and innovative ophthalmic drug screening. Featuring stable physicochemical properties, high purity and strict impurity control over related substances, residual solvents and heavy metals, it fully meets high-standard scientific research requirements. It dissolves stably in DMSO buffer solutions and supports full-process research scenarios including in vitro inflammatory cell modeling, ocular tissue culture, dry eye animal model construction and high-throughput compound screening, delivering outstanding batch uniformity and experimental repeatability.

It possesses a uniquely differentiated pharmacological mechanism distinct from conventional anti-inflammatory agents such as pranoprofen and fluorometholone. Long-term ocular oxidative stress triggers lipid peroxidation and accumulates toxic reactive aldehyde species including 4-hydroxynonenal (4-HNE) and malondialdehyde (MDA). Excessive RASP continuously activates the NF-κB inflammatory cascade, promotes massive secretion of pro-inflammatory factors in conjunctival and corneal tissues, destroys tear film stability and damages ocular surface epithelium, which serves as the fundamental cause of persistent dry eye and chronic ocular inflammation. Reproxalap specifically covalently binds and neutralizes redundant toxic aldehydes, blocking the initial inflammatory signaling at the source and inhibiting the overexpression of downstream TNF-α, IL-6 and other pro-inflammatory cytokines. Integrating anti-inflammation and anti-oxidation dual activities, it repairs damaged tear film without interfering with normal immune metabolism, avoiding hormone-related side effects such as elevated intraocular pressure and corneal injury with superior safety performance.

In clinical and scientific research applications, Reproxalap targets multiple non-infectious ocular inflammatory disorders. It is primarily applied for moderate to severe dry eye syndrome, rapidly relieving typical symptoms including ocular dryness, burning sensation, foreign body sensation, photophobia and lacrimation, and maintaining long-term ocular surface homeostasis. Multiple clinical studies verify that it effectively reduces ocular surface inflammation indexes and improves tear secretion. Beyond dry eye treatment, it is widely used in mechanism research and positive control experiments for allergic conjunctivitis, non-infectious anterior uveitis and Sjogren’s syndrome-related ocular inflammation. It also supports pharmacological research on the rare genetic ocular disease Sjogren-Larsson syndrome, demonstrating rare disease drug development potential. Benefiting from its novel mechanism, it is also a premium tool compound for cross-disciplinary research on systemic oxidative inflammation, skin lipid inflammation and neuronal oxidative damage.

In terms of raw material supply and industrial research value, Reproxalap adopts mature and stable synthetic routes with complete retention of covalent active groups. Advanced purification technology efficiently removes structural analog impurities, ensuring stable biological activity and controllable quality. Available in specifications from milligram to kilogram scale, it fully meets the R&D demands of universities, CRO laboratories and pharmaceutical enterprises. It exhibits excellent local administration tolerance without obvious irritation or toxic side effects, providing a wide safety window for long-term animal intervention experiments. With the continuously expanding global dry eye patient population and rising incidence of chronic ocular inflammation, traditional anti-inflammatory drugs are limited by side effects and high recurrence rates, making the novel RASP target a hot direction for ophthalmic innovative drug R&D. As the only marketed benchmark compound targeting RASP, Reproxalap is supported by comprehensive in vitro and in vivo activity data as well as solid clinical evidence, maintaining irreplaceable long-term scientific research value and broad market prospects in ocular pharmacology and innovative drug development.