| Description |
iNOs-IN-3 (Compound 2d) is an orally active nitric oxide synthase (iNOS) inhibitor (IC50=3.342 µM). iNOs-IN-3 shows anti-inflammatory activity and can be used in LPS-induced acute lung injury (ALI) research[1].
|
| Related Catalog |
|
| Target |
IC50: 3.342 µM (iNOS)[1]
|
| In Vitro |
iNOs-IN-3 (25 μM; 24 h) inhibits LPS-induced RAW 264.7 cells[1]. iNOs-IN-3 (12.5 μM; 24 h) can decrease the expression of iNOS[1]. Cell Viability Assay[1] Cell Line: RAW 264.7 microphages Concentration: 25 μM Incubation Time: 24 hours Result: Showed higher inhibitory activity (IC50=14.72 µM) in LPS-induced RAW 264.7 cells. Cell Viability Assay[1] Cell Line: RAW 264.7 microphages Concentration: 12.5 μM Incubation Time: 24 hours Result: Inhibited the LPS-induced mRNA expression of iNOS obviously. Cell Viability Assay[1] Cell Line: RAW 264.7 microphages Concentration: 12.5 μM Incubation Time: 24 hours Result: Inhibited the expression of TNF-α, IL-6, and IL-1β at 12.5 µM.
|
| In Vivo |
iNOs-IN-3 (oral administration; 12.5 mg/kg; once) treatment shows anti-inflammatory activity against xylene-induced ear edema in mice[1]. iNOs-IN-3 (oral administration; 3.125 mg/kg, 6.25 mg/kg, 12.5 mg/kg; once) protects against LPS-induced acute lung injury[1]. Animal Model: Xylene-induced mice[1] Dosage: 12.5 mg/kg Administration: Oral administration; 12.5 mg/kg; once Result: Showed better activity than the positive control. Animal Model: LPS-induced acute lung injury (ALI) mice[1] Dosage: 3.125 mg/kg, 6.25 mg/kg, 12.5 mg/kg Administration: Oral administration; 3.125 mg/kg, 6.25 mg/kg, 12.5 mg/kg; once Result: Attenuated the pathological lesions dose-dependently, such as decreased inflammatory infiltration and pulmonary congestion. Inhibited LPS-induced lung edema dose-dependently.
|
| References |
[1]. Li Tang, et al. Design and synthesis of new disubstituted benzoxazolone derivatives that act as iNOS inhibitors with potent anti-inflammatory activity against LPS-induced acute lung injury (ALI). Bioorg Med Chem. 2020 Nov 1;28(21):115733.
|
