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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 153 | 现货 | |
5 mg | ¥ 328 | 现货 | |
10 mg | ¥ 496 | 现货 | |
25 mg | ¥ 1,080 | 现货 | |
50 mg | ¥ 1,990 | 现货 | |
100 mg | ¥ 2,980 | 现货 | |
500 mg | ¥ 6,690 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 363 | 现货 |
产品描述 | VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of mGlu4 receptor.The EC50 of VU 0361737 is 240 nM for the human receptors. The EC50 of VU 0361737 is110 nM for rat receptors.It exhibits weak activity at mGlu5 and mGlu8 receptors, and is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS. |
靶点活性 | mGluR4 (human):240 nM(EC50), mGluR4 (rat):110 nM(EC50) |
体外活性 | VU0361737 在mGlu1、mGlu2、mGlu3、mGlu6及mGlu7受体上无活性,并在mGlu5及mGlu8受体上表现出弱活性。[1] |
体内活性 | VU0361737 在大鼠体内显示出高清除率(CL),半衰期短(T1/2 20分钟),并且显著地透过血脑屏障(脑血浆比率为4.1)。[1] |
激酶实验 | Enzyme Assays: The enzymatic activities of NAMPT and NMNAT are measured using in vitro kits and using the Two-Step Method per manufacturer's instructions. Compounds, NAMPT and/or NMNAT enzymes, and their substrates are mixed and incubated at 30°C for 1 hour. Reagents for the indicator reaction (Wst-1) are then added, and absorbance is read at 450 nm every 5 min at 30°C on a Tecan In?nite M100 multimode plate reader. |
别名 | ML-128, VU 0361737 |
分子量 | 262.69 |
分子式 | C13H11ClN2O2 |
CAS No. | 1161205-04-4 |
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: 45 mg/mL (171.3 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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