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编 号：F421394
分子式：C29H38N4O3
分子量：490.64
分子式：C29H38N4O3
分子量：490.64
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CAS No: 669076-03-3
产品详情
生物活性：
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.
体内研究：
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。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。Animal Model:C57BL/6J mice with oxygen-induced retinopathy (OIR) model
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
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.
体外研究：
JNJ-26076713 (5-5000 nM) 以剂量依赖的方式抑制 FGF2 诱导的 HUVEC 迁移。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.
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.
体内研究：
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。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。Animal Model:C57BL/6J mice with oxygen-induced retinopathy (OIR) model
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
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.
体外研究：
JNJ-26076713 (5-5000 nM) 以剂量依赖的方式抑制 FGF2 诱导的 HUVEC 迁移。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.
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