AR-13503

Names

[ Name ]:
AR-13503

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> TGF-beta/Smad >> PKC

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[In Vitro]

AR-13503 (16 小时) 抑制人脐静脉内皮细胞 (HUVEC) 管的形成，IC50 为 21 nM[1]。 AR-13503 (400 nM; 5 天) 以剂量依赖的方式减少脉络膜的发芽面积[1]。 AR-13503 (400 nM; 2 周) 以剂量依赖的方式增强猪主要 RPE 屏障功能[1]。

[In Vivo]

AR-13503 (1.25 mg/kg；腹腔注射；每天 1 次，共 5 天) 与 Aflibercept (HY-108801) 有协同作用，显著降低了异常新生血管 (NV) 形成[1]。 Animal Model: Oxygen-induced retinopathy (OIR) mice model (C57BL/6; 7-days-old)[1] Dosage: 1.25 mg/kg Administration: Intraperitoneal injection; once daily for 5 days Result: The combination group had a greater (~75%) reduction in NV than Aflibercept alone (~55%).

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₉N₃O₂

[ Molecular Weight ]:
321.37

Related Compounds

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