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M-31850 (1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis-) 是一种竞争性的 β-己糖胺酶选择性抑制剂,能够抑制人HexA (IC50:6.0 µM) 及HexB (IC50:3.1 µM)。它还能够竞争性抑制 β-N-acetyl-D-hexosaminidaseOfHex2 (Ki:2.5 µM)。
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M-31850 (1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis-) 是一种竞争性的 β-己糖胺酶选择性抑制剂,能够抑制人HexA (IC50:6.0 µM) 及HexB (IC50:3.1 µM)。它还能够竞争性抑制 β-N-acetyl-D-hexosaminidaseOfHex2 (Ki:2.5 µM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 255 | 现货 | |
10 mg | ¥ 392 | 现货 | |
25 mg | ¥ 756 | 现货 | |
50 mg | ¥ 947 | 现货 | |
100 mg | ¥ 1,566 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 376 | 现货 |
产品描述 | M-31850 (1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis-) is a potent, selective and competitive β-hexosaminidase (Hex) inhibitor(human HexA and human HexB with IC50s of 6.0 μM and 3.1 μM, respectively). IT also competitively inhibits β-N-acetyl-D-hexosaminidase OfHex2 with a Ki of 2.5 μM. |
靶点活性 | OfHex2:2.5 μM (Ki), HexA (human):6.0 µM (IC50), HexB (human):3.1 µM (IC50) |
体外活性 | M-31850能够使得成人型Tay-Sachs病(ATSD)细胞中的突变Hex A的半衰期在44°C条件下相比于在DMSO存在下加热的酶增加两倍以上。M-31850作为典型的竞争性抑制剂对Hex产生影响(随着M-31850量的增加Km增加而Vmax不受影响),其Ki为0.8 μM。M-31850对Jack Bean Hex (JBHex)和来自Streptomyces plicatus的细菌Hex (SpHex)也显示出一定的活性(分别对JBHex和SpHex的IC50为280 M和>500 M)[1]。 |
别名 | 1H-Benz[de]isoquinoline-1,3(2H)-dione, 2,2'-(iminodi-2,1-ethanediyl)bis- |
分子量 | 463.48 |
分子式 | C28H21N3O4 |
CAS No. | 281224-40-6 |
Smiles | O=C1N(CCNCCN2C(=O)c3cccc4cccc(C2=O)c34)C(=O)c2cccc3cccc1c23 |
密度 | 1.409 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 5 mg/mL (10.79 mM), when pH is adjusted to 6 with HCl. Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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