123663-49-0
123663-49-0 結(jié)構(gòu)式
基本信息
艾拉莫德及雜質(zhì)
N-(7-甲基磺胺基)-4-氧代-6-苯氧基-4H-苯并吡喃-3-基)甲酰胺
N-(7-(甲基磺酰胺O)-4-氧代-6-苯氧基-4H-苯并吡喃-3-基)甲酰胺
N-[3-(甲酰胺基)-4-氧-6-苯氧基-4H-1-苯并吡喃-7-基]甲烷磺酰胺
CS-1961
IGURATIMOD
Iguratimod >
iguratimod( R&D)
IguratiMod (T 614)
Iguratimod USP/EP/BP
N-[7-methanesulfonamido-4-oxo-6-(phenoxy)chromen-3-yl]formamide
N-(3-Formamido-4-oxo-6-phenoxy-4H-chromen-7-yl)methanesulfonamide
N-(7-(MethylsulfonaMido)-4-oxo-6-phenoxy-4H-chroMen-3-yl)forMaMide
物理化學(xué)性質(zhì)
常見問題列表
圖1為艾拉莫德的合成路線
其中：3）4-酚氧基-3-硝基苯甲醚；4）4-酚氧基-3-氨基苯甲醚；5）4-酚氧基-3-甲磺酰氨基苯甲醚；6）N-[4 -(2-氨乙?；?5-甲氧基-2-酚氧基苯基]甲磺酰胺鹽酸鹽；7）N-[4 -(2-甲酰氨乙?；?5-甲氧基-2-酚氧基苯基]甲磺酰胺；8）N-[4 -(2-甲酰氨乙?；?5-酚羥基-2-酚氧基苯基]甲磺酰胺。
有關(guān)艾拉莫德的抗風(fēng)濕藥物、作用機(jī)制、合成路線、不良反應(yīng)等是由Chemicalbook的鮑泉編輯整理。（2016-01-22）
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COX-2 20 μM (IC 50 ) |
MIF 6.81 μM (IC 50 ) |
Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC 50 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 IC 50 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 IC 50 of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro.
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.