CAS NO: | 123663-49-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Iguratimod is an antirheumatic agent, acts as an inhibitor ofCOX-2, with anIC50of 20 μM (7.7 μg/mL), but shows no effect onCOX-1. Iguratimod also inhibitsmacrophage migration inhibitory factor(MIF) with anIC50of 6.81 μM. | ||||||||||||||||
IC50& Target[1][3] |
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体外研究 (In Vitro) | Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50of 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 IC50of 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 IC50of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro[3]. | ||||||||||||||||
体内研究 (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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 374.37 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H14N2O6S | ||||||||||||||||
CAS 号 | 123663-49-0 | ||||||||||||||||
中文名称 | 艾拉莫德 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(89.03 mM;Need ultrasonic) 配制储备液
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