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COX-2-IN-34 (compound 8a) is a selective and orally active inhibitor of COX-2 , with an IC50 of 0.42 μM. COX-2-IN-34 has no gastric ulcer toxicity but has anti-inflammatory effects[1]. | [in vivo]
COX-2-IN-34 (compound 8a) (50 mg/kg for p.o., three days) shows no gastric ulceration in normal male rat model[1].
COX-2-IN-34 (50 mg/kg for s.c., three times) shows significant anti-inflammatory effects in the Carrageenan-induced rat paw edema assay model [1]. | Animal Model: | The Carrageenan-induced rat paw edema assay model[1] | | Dosage: | 50 mg/kg | | Administration: | Subcutaneous injection (s.c.) | | Result: | Expressed the reduction of edema claw volume after 0h, 1 h, 2 h, 3h, 4 h, and 6 h of carrageenan injection compared to the control group.
Exhibited superior inhibition of 42.90% and 45.95% at the 3rd and 4th hour, respectively, which was comparatively much closer in potency to that of the Celecoxib (HY-14398) group (45.18% inhibition of edema at 3h).
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| [IC 50]
COX-2: 0.42 μM (IC50) | [References]
[1] 1. 1. Min Xin, et al. Synthesis and biological evaluation of resveratrol amide derivatives as selective COX-2 inhibitors. Chemico-Biological Interactions. Volume 380, 1 August 2023, 110522. |
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