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DC-174是一种羟肟酸类口服有效的蛇毒金属蛋白酶(SVMP)小分子抑制剂,作为以XL-784为先导化合物经构效关系优化改造的候选分子,其通过羟肟酸基团螯合SVMP活性位点的锌离子,从而广谱抑制多种蛇毒(如锯鳞蝰、西部菱斑响尾蛇、马来亚蝮等)SVMP酶活性,IC50低于10 nM,并能中和蛇毒诱导的促凝血毒性。药代动力学研究表明,DC-174口服给药后约30分钟达血药峰值,但其半衰期较短(约1.41小时),通过优化多剂量给药方案可延长有效暴露时间,在严重蛇伤小鼠模型中展现出显著的生存保护效果,因此被视作开发口服蛇伤急救治疗药物的优质先导化合物。
DC-174是一种羟肟酸类口服有效的蛇毒金属蛋白酶(SVMP)小分子抑制剂,作为以XL-784为先导化合物经构效关系优化改造的候选分子,其通过羟肟酸基团螯合SVMP活性位点的锌离子,从而广谱抑制多种蛇毒(如锯鳞蝰、西部菱斑响尾蛇、马来亚蝮等)SVMP酶活性,IC50低于10 nM,并能中和蛇毒诱导的促凝血毒性。药代动力学研究表明,DC-174口服给药后约30分钟达血药峰值,但其半衰期较短(约1.41小时),通过优化多剂量给药方案可延长有效暴露时间,在严重蛇伤小鼠模型中展现出显著的生存保护效果,因此被视作开发口服蛇伤急救治疗药物的优质先导化合物。

| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mg | 待询 | 待询 | |
| 50 mg | 待询 | 待询 |
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| 产品描述 | DC-174 is an orally effective small molecule inhibitor of snake venom metalloproteinases (SVMPs) belonging to the hydroxamic acid class. As a candidate molecule optimized from the lead compound XL-784 through structure-activity relationship studies, it broadly inhibits the SVMP enzymatic activity of various snake venoms (e.g., saw-scaled viper, western diamondback rattlesnake, Malayan pit viper, etc.) with IC50 values below 10 nM by chelating the zinc ion in the SVMP active site via its hydroxamic acid group. It also neutralizes snake venom-induced procoagulant toxicity. Pharmacokinetic studies show that DC-174 reaches peak blood concentration approximately 30 minutes after oral administration but has a short half-life (approx. 1.41 hours). Optimized multi-dose regimens can prolong effective exposure time, demonstrating significant survival protection effects in severe snakebite mouse models, thus positioning it as a promising lead compound for developing oral emergency snakebite treatments. |
| 分子量 | 419.47 |
| 分子式 | C15H21N3O7S2 |
| Smiles | O=S(N1C[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OC)C=C2)=O)CC1)(C3CC3)=O |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 |
对于不同动物的给药剂量换算,您也可以参考 更多