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PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), with an IC 50 value of 0.52 µM. In vitro studies show that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α and impedes retinal vasculature permeability induced by both VEGF and TNF-α. [1]
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $2,140 | 6-8 weeks | |
50 mg | $2,785 | 6-8 weeks | |
100 mg | $3,520 | 6-8 weeks |
Description | PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), with an IC 50 value of 0.52 µM. In vitro studies show that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α and impedes retinal vasculature permeability induced by both VEGF and TNF-α. [1] |
In vitro | PKC-IN-4 (compound 7l) demonstrates VEGF-induced endothelial permeability with an EC50 of 0.071 μM [1]. |
In vivo | PKC-IN-4, administered at doses of 10 mg/kg intravenously (i.v.) and 20 mg/kg orally (p.o.), demonstrates oral activity with an oral bioavailability of 81.7% in CD-1 mice. This compound, when tested, exhibited favorable pharmacokinetic (PK) parameters, substantiating its effectiveness and potential for further development. |
Molecular Weight | 379.52 |
Formula | C21H25N5S |
Cas No. | 2636771-29-2 |
Storage | Shipping with blue ice. |
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