| 中文名称: | GLPG0187 | ||||
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| 英文名称: | GLPG0187 | ||||
| 别名: | 3-[[2,5-二甲基-6-[4-(5,6,7,8-四氢-1,8-萘啶-2-基)-1-哌啶基]-4-嘧啶基]氨基]-N-[(4-甲氧基苯基)磺酰基]-L-丙氨酸 GLPG0187;GLPG-0187 | ||||
| CAS No: | 1320346-97-1 | 分子式: | C29H37N7O5S | 分子量: | 595.71 |
| CAS No: | 1320346-97-1 | ||||
| 分子式: | C29H37N7O5S | ||||
| 分子量: | 595.71 | ||||
基本信息
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产品编号：G10411 |
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产品名称：GLPG0187 |
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CAS: |
1320346-97-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
595.71 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.6787mL |
8.3933mL |
16.7867mL |
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5mM |
0.3357mL |
1.6787mL |
3.3573mL |
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10mM |
0.1679mL |
0.8393mL |
1.6787mL |
生物活性
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产品描述 |
一种广谱的integrin受体拮抗剂，具有抗肿瘤活性;抑制αvβ1-integrin的IC50值为1.3nM。 |
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靶点/IC50 |
1.3nM (αvβ1) |
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体外研究 |
In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors with IC50s of 1.3, 3.7, 2.0, 1.4, 1.2, 7.7nM for αvβ1,αvβ3, αvβ5, αvβ6,αβ8, andα5β1. GLPG0187 is a potent inhibitor of osteoclastic bone resorption and angiogenesis. Treatment with GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio, rendering the cells a more epithelial, sessile phenotype.GLPG0187 dose-dependently diminishes the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells.GLPG0187 treatment results in cell rounding and clumping.GLPG0187 demonstrates a dose-dependent significant reduction in tumour cell migration. GLPG0187 at all concentrations significantly reduces cell proliferation. |
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体内研究 |
Blocking αv-integrins by GLPG0187 markedly reduces their metastatic tumor growth. Bone tumor burden is significantly lower and the number of bone metastases/mouse is significantly inhibited. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited. |
推荐实验方法(仅供参考)
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细胞实验: |
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Tumour cell proliferation is determined using the MTS assay. PC3 cells are seeded at 10,000 cells/well in 96 well plates containing either GLPG0187 (0.5, 5, or 50ng/mL), vehicle or media control, then cultured in 100µL medium for 24 hr. Cell proliferation is analysed using 20µL MTS dye incubated for 3 hr at 37℃ in the dark.Absorbance from each well (6/treatment) is quantified at 490nm and the mean fluorescence calculated. The assay is repeated at 48,72 and 96 hr, on three independent occasions. |
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动物实验: |
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Mice: The effect of GLPG0187 on bone loss is evaluated in 3-month-old castrated male mice after 4 weeks of treatment with dosing starting immediately after castration (preventive protocol).Two different modes of administration are used: either subcutaneous twice daily with 10, 30, or 100mg/kg of GLPG0187, either oral, twice daily with 30, 100, or 300mg/kg of GLPG0187. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
