中文名称: PD 123319
英文名称: PD 123319
CAS No: 130663-39-7
分子式: C31H32N4O3
分子量: 508.61
P10996 PD 123319 ≥98% (psaitong)
包装规格:
25mg in glass bottle
产品描述:

基本信息

产品编号:

P10996

产品名称:

PD 123319

CAS:

130663-39-7

 

储存条件

粉末

-20℃

四年

分子式:

C31H32N4O3

溶于液体

-80℃

二年

分子量:

508.61

 

 

化学名: 

(S)-1-(4-(dimethylamino)-3-methylbenzyl)-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid

Solubility (25°C):

 

体外:

 

DMSO

100mg/mL (196.61mM)

Ethanol

100mg/mL (196.61mM)

Water

100mg/mL (196.61mM)

体内(现配现用):

Saline

30mg/mL

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

1.9661mL

9.8307mL

19.6614mL

5mM

0.3932mL

1.9661mL

3.9323mL

10mM

0.1966mL

0.9831mL

1.9661mL

50mM

0.0393mL

0.1966mL

0.3932mL

 

生物活性

产品描述

一种血管紧张素II受体拮抗剂,IC50为34nM。

靶点

34nM (AT2 Receptor) 

 

体外研究

PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues.125I-AII specifically label two classes of binding sites for AII in a membrane preparation of bovine adrenal glomerulosa cells.The first class (DuP753 sensitive) represents approximately 85% of the total binding sites for AII and possesses a high affinity (IC50 of 92.9nM) for DuP-753.PD-123319 does not have any effect on 125I-AII binding to this site. The second class of binding sites is more sensitive to PD-123319,with an IC50 of 6.9nM,and has a much lower affinity for DuP-753 (IC50 around 10 microM).

体内研究

PD123319对脑血流量的自我调节没有影响。急性AT2受体阻断不影响脑血流自动调节功能。PD 123319静脉给药导致了高血压大鼠中瞬时的剂量依赖性的MAP增加,3毫克/千克的PD123319导致MAP维持约为7.4分钟。

 

推荐实验方法(仅供参考)

动物实验:

 

The lower limit of CBF autoregulation is studied in 16 SHR.Eight animals receive PD 123319,while eight serve as controls.PD 123319 or saline is administered intravenously,and the BP is allowed to stabilise for 10 minutes after the injection and prior to the commencement of the autoregulation study.Haemorrhagic hypotension is subsequently induced by withdrawing blood into a syringe.By this means,BP is reduced stepwise to the lowest obtainable level.Throughout the study,CBF is measured at 10 to 15 mmHg BP intervals.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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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

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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

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  • 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):