Iguratimod

Research use only, not for human use.

A novel disease-modifying antirheumatic drug that inhibits NF-kappaB (NF-κB) p65 subunit (RelA) phosphorylation and nuclear translocation without affecting IKBα degradation.

A novel disease-modifying antirheumatic drug that inhibits NF-kappaB (NF-κB) p65 subunit (RelA) phosphorylation and nuclear translocation without affecting IKBα degradation; inhibits LPS-stimulated production of TNF-α, IL-6, and IL-8 with decreasing mRNA levels (IL-6 and IL-8); mainly targets Act1 to disrupt the interaction between Act1 and TRAF5 and IKKi in the IL-17 pathway of synoviocytes; also exhibts selective MIF inhibition in vitro and in vivo.Rheumatoid Arthritis Approved(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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TT-614

Apoptosis

NF-κB

COX-2|MIF

Inflammation/Immunology

Rheumatoid Arthritis

123663-49-0

374.3679

C17H14N2O6S

>98% (HPLC)

10 mM in DMSO

O=CNC1=COC2=C(C=C(OC3=CC=CC=C3)C(NS(=O)(C)=O)=C2)C1=O

Methanesulfonamide, N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-

(-20℃)

With Ice Pack

≥ 2 years