AMI-1
产品说明书
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同义名 : | - |
| CAS号 : | 20324-87-2 | |
| 货号 : | A201673 | |
| 分子式 : | C21H14N2Na2O9S2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 548.45 | |
| MDL号 : | MFCD00068249 | |
| 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 : |
H2O: 60 mg/mL(109.4 mM)，配合低频超声，并水浴加热至45℃助溶 |
| 生物活性 | |||
|---|---|---|---|
| 描述 | AMI-1 is a specific arginine methyltransferase inhibitor (a pan-PRMT inhibitor) with IC50 value of 1.63μM for PRMT1. It inhibited methylation of GFP-Npl3 and cellular proteins. Dose-dependent reduction of nuclear receptor-mediated transactivation, including an estrogen response element (ERE) and an androgen response element, could be observed in MCF7 cells transfected with a luciferase reporter post treatment with AMI-1 at 5, 50 and 100μM[3]. AMI-1 inhibited the expression of COX2 on mRNA level in TGF-β–stimulated cells. AMI-1 (50μl at a concentration of 0.1 mg/ml in PBS 2h before OVA challenge) administered to AIPI (Ag-induced pulmonary inflammation) rats reduced COX2 production and humoral immune response, and it abrogated mucus secretion and collagen generation[4]. | ||
| 作用机制 | AMI-1 inhibits arginine methylation by inserting into the arginine-binding pocket.[3] | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01103518 | Amenorrhea Dy... 展开 >>smenorrhea Menstruation Disturbances Hyperandrogenism 收起 << | Phase 4 | Unknown | January 2011 | Brazil ... 展开 >> Hospital das Clínicas de Teresópolis Teresópolis, Rio de Janeiro, Brazil, 25976-016 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.82mL 0.36mL 0.18mL |
9.12mL 1.82mL 0.91mL |
18.23mL 3.65mL 1.82mL |
| 参考文献 |
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