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PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]
PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 14,900 | 6-8周 | |
50 mg | ¥ 19,420 | 6-8周 | |
100 mg | ¥ 24,625 | 6-8周 |
产品描述 | PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1] |
体外活性 | PKC-IN-4 (compound 7l) shows VEGF - induced endothelial permeability with an EC 50 of 0.071 μM [1]. |
体内活性 | PKC-IN-4 (10 mg/kg for i.v.; 20 mg/kg for p.o.) shows orally active with oral bioavailability of 81.7% [1]. Animal Model: Animal Model: CD-1 mice [1] Dosage: 10, 20 mg/kg Administration: 10 mg/kg for i.v.; 20 mg/kg for p.o. Result: Showed good PK parameters with oral bioavailability of 81.7%. |
分子量 | 379.52 |
分子式 | C21H25N5S |
CAS No. | 2636771-29-2 |
存储 | Shipping with blue ice. |
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