普马司他
普马司他 性质
| 熔点 | 149.8° |
|---|---|
| 密度 | 1.377±0.06 g/cm3(Predicted) |
| 储存条件 | room temp |
| 溶解度 | 在水中的溶解度为15mg/mL（澄清溶液） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.25±0.23(Predicted) |
| 颜色 | 白色至米色 |
| 水溶解性 | H2O: 15mg/mL (clear solution) |
| InChI | 1S/C18H21N3O5S2.ClH/c1-18(2)16(17(22)20-23)21(11-12-27-18)28(24,25)15-5-3-13(4-6-15)26-14-7-9-19-10-8-14;/h3-10,16,23H,11-12H2,1-2H3,(H,20,22);1H/t16-;/m0./s1 |
| InChIKey | UQGWXXLNXBRNBU-NTISSMGPSA-N |
| SMILES | Cl.CC1(C)SCCN([C@H]1C(=O)NO)S(=O)(=O)c2ccc(Oc3ccncc3)cc2 |
普马司他 用途与合成方法
|
MMP-9 5 nM (IC 50 ) |
MMP-9 0.26 nM (Ki) |
MMP-2 0.05 nM (Ki) |
MMP-1 79 nM (IC 50 ) |
MMP-3 6..3 nM (IC 50 ) |
MMP-3 0.3 nM (Ki) |
Prinomastat (AG3340; 0.1-1 µg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat.
Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat (AG3340).
Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. As anticipated, the migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells.The effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat in C57MG/Wnt1 cells.
Western Blot Analysis
| Cell Line: | C57MG/Wnt1 cells |
| Concentration: | 0.1 µg/mL, 1 µg/mL |
| Incubation Time: | 4 days |
| Result: | A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells. |
In a human fibrosarcoma mouse model (HT1080), the mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumour inoculation. Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition, with a short T 1/2 of 1.6 hours.
安全信息
| 危险品标志 | T |
|---|---|
| 危险类别码 | 60-61 |
| 安全说明 | 53-45 |
| WGK Germany | 3 |
| 存储类别 | 6.1C - 可燃，急性毒性 类别3 毒性化合物或者引起慢性影响的化合物 |
| 危险性类别 | 生殖毒性 类别1B |
普马司他 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-12-22 | HY-12170A | 普马司他 | 192329-42-3 | 1mg | 1250 |
| 2025-12-22 | HY-12170A | 普马司他 | 192329-42-3 | 5mg | 3060 |
