JNJ-26076713

JNJ-26076713 is a potent and orally active alpha V integrin antagonist with IC50 values of 2.3 nM and 6.3 nM for alpha(V)beta(3) and alpha(V)beta(5), respectively. JNJ-26076713 inhibits retinal neovascularization[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> Cytoskeleton >> Integrin

αvβ3:2.3 nM (IC50)

αvβ5:6.3 nM (IC50)

JNJ-26076713 (5-5000 nM) 以剂量依赖的方式抑制 FGF2 诱导的 HUVEC 迁移[1]。 JNJ-26076713 (0.1, 1, 和 10 μg) 以剂量依赖的方式抑制鸡胚绒毛尿囊膜 (CAM) 模型的血管生成[1].

JNJ-26076713 (30-120 mg/kg; i.g.; 每天两次, 连续5天; 氧诱导视网膜病变 (OIR) 模型C57BL/6J 小鼠) 以剂量依赖的方式抑制视网膜新生血管[1]。 JNJ-26076713 (60 mg/kg; i.g.; 每天两次, 连续5天; 糖尿病 Long-Evans 大鼠) 抑制与糖尿病相关的视网膜血管通透性和白细胞瘀血的增加[1]。 Animal Model: C57BL/6J mice with oxygen-induced retinopathy (OIR) model[1] Dosage: 30, 60, and 120 mg/kg Administration: Oral gavage, twice daily for 5 days Result: Inhibited retinal neovascularization with 33, 43, and 67% inhibition of neovascularization at 30, 60, and 120 mg/kg, respectively. Animal Model: Diabetic Long-Evans rats[1] Dosage: 60 mg/kg Administration: Oral gavage, twice daily for 5 days Result: Reduced leukocyte adhesion with 48% and inhibited retinal vascular permeability in streptozotocin diabetic rats.

[1]. Santulli RJ, et, al. Studies with an orally bioavailable alpha V integrin antagonist in animal models of ocular vasculopathy: retinal neovascularization in mice and retinal vascular permeability in diabetic rats. J Pharmacol Exp Ther. 2008 Mar;324(3):894-901.