| 中文名称: | CMPD101 | ||||
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| 英文名称: | CMPD101 | ||||
| CAS No: | 865608-11-3 | 分子式: | C24H21F3N6O | 分子量: | 466.46 |
| CAS No: | 865608-11-3 | ||||
| 分子式: | C24H21F3N6O | ||||
| 分子量: | 466.46 | ||||
基本信息
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产品编号：C10936 |
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产品名称：CMPD101 |
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CAS: |
865608-11-3 |
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： |
466.46 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
' mg/mL |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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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 |
2.1438mL |
10.7190mL |
21.4381mL |
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5mM |
0.4288mL |
2.1438mL |
4.2876mL |
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10mM |
0.2144mL |
1.0719mL |
2.1438mL |
生物活性
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产品描述 |
一种高效、高选择性、膜透性的 GRK2/3 小分子抑制剂，IC50 分别为 18nM 和 5.4nM。CMPD101 针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50 值分别为 3.1μM，2.3μM，1.4μM 和 8.1μM。CMPD101 可用于心衰疾病的研究。 |
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靶点/IC50 |
GRK2 18nM (IC50) |
GRK3 5.4nM (IC50) |
PKCα |
ROCK2 |
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体外研究 |
CMPD101 (100μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line.CMPD101 (3-30μM; pre-30 minutes) produced a robust phosphorylation of Ser375, which is partially inhibited by pretreatment of cells for 30 minutes with 3μM Cmpd101 and fully blocked by pretreatment with 30μM Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues.CMPD101 (3-30μM;pre-30 minutes) does not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30μM, this compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs. Western Blot Analysis |
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Cell Line: |
HEK 293 cells stably expressing HA-tagged rat MOPr |
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Concentration: |
3μM, 30μM |
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Incubation Time: |
Pre-30 minutes |
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Result: |
Surpressed Ser375 expression completely at a high dose. |
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Western Blot Analysis |
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Cell Line: |
HEK 293 cells stably expressing HA-tagged rat MOPr |
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Concentration: |
3μM, 30μM |
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Incubation Time: |
Pre-30 minutes |
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Result: |
Had no effect on DAMGO-induced p-ERK1/2 and p-Elk-1 expression. |
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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 )
