GI254023X
产品说明书
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同义名 : | SRI028594;GI4023 |
| CAS号 : | 260264-93-5 | |
| 货号 : | A164330 | |
| 分子式 : | C21H33N3O4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 391.504 | |
| MDL号 : | MFCD19381832 | |
| 存储条件： |
Pure form Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(268.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | In experiments on cellular models, GI254023X markedly inhibits the baseline shedding of RAGE at a concentration of 25 μM, and this inhibitory effect persists, albeit to a lesser extent, at 1 μM. The compound shows a modest reduction in RAGE shedding at a concentration of 100 nM. Distinguishing between various proteinases in vitro, GI254023X exhibits selectivity, demonstrating an IC50 of 541 nM against ADAM17 and more potent inhibition against ADAM10 (IC50=5.3 nM) and MMP9 (IC50=2.5 nM)[1]. The shedding of CXCL16 is obstructed by inhibitors of ADAM proteases, such as GI254023x. A2780 cells, when treated with the ADAM-10/ADAM-17 inhibitor TAPI-2 along with GI254023x, a selective inhibitor for ADAM-10, reveal a significant difference in the expression levels of ADAM-10 mRNA, being almost 9.8 times higher than that of ADAM-17. Moreover, GI254023x efficiently prevents the shedding of CXCL16 from the cell surface, surpassing the effectiveness of TAPI-2[2]. Utilizing the specific inhibitor for ADAM10 (α-secretase), GI254023X, at a concentration of 5 mM on serum/glucose-depleted slices results in a noticeable rise in PI counts compared to slices treated with DMSO (the carrier)[3]. | ||
| 作用机制 | GI254023X has an improved fit to the specificity pocket of ADAM10 as compared to that of ADAM17. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.26mL |
12.77mL 2.55mL 1.28mL |
25.54mL 5.11mL 2.55mL |
| 参考文献 |
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