tcsc0617 Iguratimod

Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC₅₀ of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC₅₀ of 6.81 μM.

IC50 & Target: IC50: 20 μM (COX-2)^[1], 6.81 μM (MIF)^[3]

In Vitro: Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC₅₀ of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod (0.1, 1, 10 μg/mL) inhibits bradykinin-stimulated PGE2 release from fibroblasts. Iguratimod suppresses the COX activity from bradykinin stimulated fibroblasts in a concentration-dependent manner, with an IC₅₀ of 48 μg/mL. Iguratimod (10 and 30 μg/mL) also dose-dependently inhibits COX-2 mRNA levels^[1]. In addition, Iguratimod potently inhibits macrophage migration inhibitory factor (MIF) with an IC₅₀ of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro^[3].

In Vivo: Iguratimod (5 or 20 mg/kg) shows analgesic effect, significantly improves the pain withdrawal threshold of the left hind paw in dose-dependent manner in rats. Iguratimod (5 or 20 mg/kg) reduces the elevation of pERK1/2 and c-Fos in the spinal cord induced by cancer cell inoculation. Iguratimod also dose-dependently decreases the IL-6 levels in rats. In Iguratimod-treated rats, the activity of osteoclasts is weaker than the control group^[2]. Iguratimod (20 mg/kg i.p.) shows significantly increased survival in BALB/c mice that are vulnerable to endotoxemia, and attenuates TNFα release measured in serum isolated 90 min post-LPS administration in wild-type C57BL/6 mice^[3].