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| 产品描述 |
| GSK484 is a potent PAD-4 inhibitor (Protein-arginine deiminase type-4). GSK484 potently binds to the low-calcium form of PAD4 in a reversible manner (IC50 of 50 nM) and appears to be competitive with substrate. GSK484’s selectivity for PAD4 over PAD1-3 was shown in cells and also confirmed with recombinant enzymes. This probe is an inhibitor of cellular citrullination in primary neutrophils, and further phenotypic profiling has confirmed its ability to inhibit NET formation in both mouse and human neutrophils. GSK484 exhibits favourable pharmacokinetic profiles, with low-moderate clearance, and good volume of distribution and half-life in mouse and rat, and has suitable a PK profile for use as a potential in vivo tool. |
| 化学结构 |
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| 化学名称 |
| ((3S,4R)-3-amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone |
| SMILES Code |
| O[C@@H]1CCN(C[C@@H]1N)C(C2=CC3=C(C(OC)=C2)N(C)C(C4=CC5=C(N4CC6CC6)C=CC=C5)=N3)=O |
| 基本信息 |
产品编号:XM127
产品名称:GSK484
别名:GSK484; GSK-484; GSK 484.
CAS#:1652591-81-5
分子式:C27H31N5O3
精确分子量:473.2427
分子量:473.577
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| 物化性质 |
外观: 固体粉末
纯度: >98%
运输信息: 非危险化学品，适于常温或冰袋运输。
储存条件: 低温，干燥，避光。
溶解性: 溶于DMSO, 不溶于水
储存期限:3年 -20℃固体储存
2 年 -80℃ 溶液储存 |
该产品只供科研使用，不能给病人提供。
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