CAS NO: | 287405-51-0 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
Apratastat 是一种口服活性,有效且可逆的肿瘤坏死因子-α 转换酶 TACE 和基质金属蛋白酶 MMPs 的双重抑制剂。Apratastat 可以在体外,离体和体内有效抑制 TNF-α 的释放,体外和离体的 IC50 分别为 144 ng/mL和 81.7 ng/mL。
Cas No. | 287405-51-0 |
别名 | N-羟基-4-[[4-[(4-羟基-2-丁炔基)氧基]苯基]磺酰基]-2,2-二甲基-3-硫代吗啉甲酰胺,TMI-005 |
化学名 | (3S)-N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-3-thiomorpholinecarboxamide |
Canonical SMILES | CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1 |
分子式 | C17H22N2O6S2 |
分子量 | 414.5 |
溶解度 | 10mg/mL in ethanol, 25mg/mL in DMSO, or in DMF |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
文献引用 | |
产品描述 | TMI-005 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-α converting enzyme (ADAM17/TACE), matrix metalloproteinase-1 (MMP-1), and MMP-13 (IC50s = 20, 33, and 8.1 nM, respectively).[1] It inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 144 ng/ml).[2] TMI-005 (25 μM) reduces basal and ionizing radiation-induced secretion of the ADAM17/TACE substrates ALCAM and amphiregulin from A549 and NCI H125 cells.[3]It inhibits proliferation of A549 cells when used at concentrations of 25 and 50 μM and sensitizes A549 and NCI H125 cells to ionizing radiation at 25 μM. TMI-005 (25 mg/kg twice per day) reduces tumor growth in an A549 mouse xenograft model when administered in combination with ionizing radiation. Reference: |