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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1232030-35-1
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥730.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥650.0 |
| 规格： | 10 mg | 产品价格： | ￥1100.0 |
| 规格： | 50 mg | 产品价格： | ￥2900.0 |
| 规格： | 100 mg | 产品价格： | ￥5100.0 |
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FRAX486
CAS No. : 1232030-35-1
MCE 国际站：FRAX486
产品活性：FRAX486 是一种 PAK抑制剂，对 PAK1，PAK2 和 PAK3 的 IC50 值分别为 14，33 和 39 nM。
研究领域：Cell Cycle/DNA Damage | Cytoskeleton
作用靶点：PAK
In Vitro: In vitro kinase assays using pure enzymes reveal IC50s for FRAX486 between 10-100 nM for PAK1-3, while the IC50 of 779 nM for PAK4 is just below the micromolar range. For FRAX486, an EC50 value of 500 nM has been reported from cells (5-50 fold higher than IC50). FRAX486 (30 μM) inhibits endothelin-1 and -2 induced contractions. In WPMY-1 cells, FRAX486 (24 h) induces concentration-dependent (1-10 μM) degeneration of actin filaments. This is paralleled by attenuation of proliferation rate, being observed from 1 to 10 μM FRAX486. Cytotoxicity of FRAX486 in WPMY-1 cells is time- and concentration-dependent. FRAX486 significantly reduces the relative proliferation rate in the remaining populations of WPMY-1 cells. While 68% of solvent-treated (24 h) cells shows proliferation, proliferation rate after application of FRAX486 (1-10 μM, 24 h) ranges around 45%. FRAX486 (1-10 μM, 24 h) causes concentration-dependent degeneration of actin filaments. Actin filaments in solvent-treated control cells are arranged to bundles, forming long and thin protrusions, with elongations from adjacent cells overlapping each other. FRAX486 in concentrations of 1 μM causes partial loss of actin organization, including regressing degree of actin polymerization and degeneration of protrusions. FRAX486 in concentrations of 5 or 10 μM causes complete breakdown of filament organization, resulting in a rounded cell shape without protrusions.
In Vivo: FRAX486 displays the highest penetrance of blood–brain barrier in DISC1-knockdown C57BL/6 mice. Daily administration of FRAX486, but not that of vehicle, between P35 and P60 blocks the exacerbated spine loss during adolescence. In addition to the significant blockade of spine elimination, a trend of enhanced spine generation is observed by treatment with FRAX486. FRAX486 treatment ameliorates a deficit in prepulse inhibition in adulthood.
相关产品：Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Targeted Diversity Library | Membrane Protein-targeted Compound Library | Fingolimod hydrochloride | 5-Aminosalicylic Acid | PF-3758309 | IPA-3 | NVS-PAK1-1 | FRAX597 | G-5555 | GNE 2861 | FRAX1036 | LCH-7749944 | Padnarsertib | MRIA9 | AZ13705339 hemihydrate | AZA197 | Fingolimod-d4 | Fingolimod-d4 hydrochloride | G-9791 | Gardenin A | KY-04031 | Mesalamine impurity P | NVS-PAK1-C | PAK1-IN-1 | PAK4-IN-1 | PAK4-IN-2
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文献和实验HPTLC system equipped with a sample applicator Linomat IV and TLC scanner and integration software CAT 4.0. In HPLC C18 (ODS) reverse phase column; water 486 UV detector; mobile phase, water/methanol (35:65, HPLC grade) + 0.1% acetic acid
后，测量宫腔深度，以了解宫腔缩小情况。 （五）注意事项 1． 出血多时，可于宫旁注射缩宫素（催产素）10u。 2． 宫颈扩张后必须先刺破羊膜，使羊水流尽后才能注射催产素，以免发生羊水栓塞。 3． 胎儿骨骼通过宫颈管时要以纵轴方向牵出，不宜用暴力，以免损伤宫颈管。 4． 术后注意事项同人流负压吸引术。 人工流产并发症及其防治 编辑本段 回目录 一般情况下不发生并发症。但遇到有高危因素（年龄35岁；有近期人流史
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