(rac)-AR-13503

(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503. AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice ^{[1] [2]}.

In Vivo, AR-13503 (1.25 mg/kg; i.p.; once daily for 5 days) in collaboration with Aflibercept, significantly decreases the development of aberrant neovascularization (NV)^[1].

In Vitro, AR-13503 (16 h) inhibits human umbilical vein endothelial cell (HUVEC) tube formation, with an IC₅₀ value of 21 nM^[1]. AR-13503 (400 nM; 5 d) decreases the sprouting area of the choroidal in a dose-dependent manner^[1]. AR-13503 (400 nM; 2 weeks) enhances primary porcine RPE barrier function in a dose-dependent manner^[1].

References:
[1]. Ding J, et al. ROCK/PKC inhibitor AR-13503 inhibits angiogenesis and protects the barrier function of retinal pigment epithelium[J]. Investigative Ophthalmology & Visual Science, 2018, 59(9): 205-205.
[2]. Carbajal K, et al. AR-13503 Enhances the efficacy of aflibercept in a mouse model of proliferative diabetic retinopathy[J]. Investigative Ophthalmology & Visual Science, 2018, 59(9): 200-200.