| 中文名称: | PD176252 | ||||
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| 英文名称: | PD176252 | ||||
| 别名: | PD-176252 | ||||
| CAS No: | 204067-01-6 | 分子式: | C32H36N6O5 | 分子量: | 584.67 |
| CAS No: | 204067-01-6 | ||||
| 分子式: | C32H36N6O5 | ||||
| 分子量: | 584.67 | ||||
基本信息
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产品编号： |
P10998 |
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产品名称： |
PD176252 |
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CAS: |
204067-01-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃（氮气储存） |
6个月 |
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分子量： |
584.67 |
-20℃（氮气储存） |
1个月 |
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化学名： |
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Solubility (25°C)： |
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体外:
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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 |
1.7104mL |
8.5518mL |
17.1037mL |
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5mM |
0.3421mL |
1.7104mL |
3.4207mL |
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10mM |
0.1710mL |
0.8552mL |
1.7104mL |
生物活性
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产品描述 |
一种有效的 BB1 和 BB2 拮抗剂，能够抑制人 BB1 和 BB2 受体和大鼠 BB1 和 BB2 受体活性，Ki 值分别为 0.17nM，1nM 和 0.66nM，16nM;PD176252 同时为 FPR1/FPR2 的激动剂，在 HL-60 细胞中，EC50 值分别为 0.31 和 0.66μM。 |
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靶点 |
Ki:0.17nM (Human BB1 receptor),0.66nM (Rat BB1 receptor),1nM (Human BB2 receptor),16nM (Rat BB2 receptor) EC50:0.31μM (FPR1),0.66μM (FPR2) |
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体外研究 |
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17nM and 1nM for human BB1 and BB2 receptors,and 0.66nM,16nM for Rat BB1 and BB2 receptors,respectively.PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB1 or BB2 receptors expressed in CHO cells,with the appKBs of 4.0nM or 13nM,and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB1 or BB2 receptors,with appKBs of 2.3nM and 36nM,respectively.PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2),with EC50s of 0.31 and 0.66μM in HL-60 cells.PD176252 activates Ca2+mobilization in HL-60 cells transfected with human FPRs (EC50,0.72±0.21μM).PD176252 inhibits little specific 125I-gastrin releasing peptide binding to NCI-H345 cells at 1nM and suppresses almost all specific bindings at 1000nM,with an IC50 of 30nM.PD176252 (10,30μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC50s of 7 and 5μM. |
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体内研究 |
PD176252 (1,10μg,p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice. |
推荐实验方法(仅供参考)
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细胞实验: |
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Growth studies in vitro are conducted using the MTT colorimetic assays.NCI-H1299 cells (104/well) are placed in SIT medium and various concentrations of PD176252 or PD168368 added.After 4 days,MTT is added.After 4h,150μL of DMSO is added.After 16h,the optical density at 570nm is determined. |
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动物实验: |
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Mice Female athymic Balb/c nude mice,4-5 weeks old,are housed in a pathogen-free temperature controlled isolation room,with a diet consisting of autoclaved rodent chow and autoclaved water given ad libitum.NCI-H1299 cells (1×107) are injected into the right flank of each mouse by subcutaneous injection.Palpable tumors are observed in approximately 90% of the mice after 1 week.Polyethylene glycol (PEG,100μL) or PD176252 (10 or 1μg in 100μL of PEG 400) are injected daily by gavage.The tumor volume (height×width×depth) is determined weekly by calipers and recorded. |
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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 )
