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Iguratimod

CAS No. : 123663-49-0

MCE 站：Iguratimod

产品活性：Iguratimod 是一种抗风湿剂，能够有效地抑制 COX-2 的活性，IC₅₀ 值为 20 μM (7.7 μg/mL)，而对 COX-1 无作用；Iguratimod 同时为巨噬细胞移动抑制因子 (MIF) 抑制剂，IC₅₀ 值为 6.81 μM。

研究领域：Immunology/Inflammation

作用靶点：COX

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. In addition, Iguratimod potently inhibits macrophage migration inhibitory factor (MIF) with an IC₅₀ of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro.

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. 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.

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