中文名称: PD176252
英文名称: PD176252
CAS No: 204067-01-6
分子式: C32H36N6O5
分子量: 584.67
P10998 PD176252 ≥98% (psaitong)
包装规格:
5mg 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℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):