中文名 | 艾拉莫德 |
英文名 | Iguratimod |
别名 | 艾拉莫德 艾拉莫德及杂质 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 |
英文别名 | T 614 Ailamode Iguratimod IGURATIMOD IguratiMod (T 614) N-[7-methanesulfonamido-4-oxo-6-(phenoxy)chromen-3-yl]formamide N-(7-(MethylsulfonaMido)-4-oxo-6-phenoxy-4H-chroMen-3-yl)forMaMide N-[3-(formylamino)-4-oxo-6-phenoxy-4H-chromen-7-yl]methanesulfonamide 3-(Formylamino)-7-(methylsulfonylamino)-6-phenoxy-4H-1-benzopyran-4-one N-[3-(Formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]methanesulfonamide |
CAS | 123663-49-0 |
EINECS | 808-127-0 |
化学式 | C17H14N2O6S |
分子量 | 374.37 |
InChI | InChI=1/C17H14N2O6S/c1-26(22,23)19-13-8-15-12(17(21)14(9-24-15)18-10-20)7-16(13)25-11-5-3-2-4-6-11/h2-10,19H,1H3,(H,18,20) |
密度 | 1.52±0.1 g/cm3(Predicted) |
熔点 | 238.0 to 242.0 °C |
沸点 | 580.6±60.0 °C(Predicted) |
闪点 | 304.9°C |
蒸汽压 | 1.8E-13mmHg at 25°C |
溶解度 | DMSO (微溶) |
折射率 | 1.673 |
酸度系数 | 5.58±0.20(Predicted) |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
外观 | 固体 |
颜色 | White to Off-White |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.671 ml | 13.356 ml | 26.712 ml |
5 mM | 0.534 ml | 2.671 ml | 5.342 ml |
10 mM | 0.267 ml | 1.336 ml | 2.671 ml |
5 mM | 0.053 ml | 0.267 ml | 0.534 ml |
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