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PD176252  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（115mg/mL 超声）
产品描述：基本信息 产品编号： P10998 产品名称： PD176252 CAS: 204067-01-6   储存条件 粉末 -20℃ 四年 分子式： C32H36N6O5 溶于液体 -80℃（氮气储存） 6个月 分子量： 584.67 -20℃（氮气储存） 1个月 化学名：  (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 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。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.7104mL 8.5518mL 17.1037mL 5mM 0.3421mL 1.7104mL 3.4207mL 10mM 0.1710mL 0.8552mL 1.7104mL   生物活性 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。 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)   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. 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) 细胞实验:   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.   动物实验:   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.
保存条件：-20℃

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