中文名称: WHI-P97
英文名称: WHI-P97
CAS No: 211555-05-4
分子式: C16H13Br2N3O3
分子量: 329.39
W10039 WHI-P97 ≥98% (psaitong)
包装规格:
100mg in glass bottle
溶解性:
溶于DMSO(5.88mg/mL 超声)
产品描述:

基本信息

产品编号:

W10039

产品名称:

WHI-P97

CAS:

211555-05-4

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C16H13Br2N3O3

溶于液体

-80℃

6个月

分子量:

329.39

-20℃

1个月

化学名: 

WHI-P 974-(3',5'-Dibromo-4-hydroxyphenyl)amino-6,7-dimethoxyquinazoline

Solubility (25°C):

 

体外:

 

DMSO

8mg/mL (17.57mM)

Ethanol

Insoluble

Water

Insoluble

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

2.1973mL

10.9866mL

21.9732mL

5mM

0.4395mL

2.1973mL

4.3946mL

10mM

0.2197mL

1.0987mL

2.1973mL

 

生物活性

产品描述

一种有效的选择性JAK-3抑制剂。WHI-P97在动物模型中有效预防过敏性哮喘的发展。

靶点

JAK3 11μM (IC50)

 

体外研究

WHI-P97 inhibits the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcεRI crosslinking by >90% at low micromolar concentrations.WHI-P97 (30μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells.

体内研究

WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5μg/kg to 50mg/kg,and LD10 is not reached at a 50mg/kg dose level when administered as a single i.p.or i.v.bolus dose.WHI-P97 (i.v.injection;40mg/kg;single dose) has an elimination half-life (t1/2) of 58.9 min and systemic clearance (CL) of 891ml/h/kg in CD-1 mice and a t1/2 of 84.2 min and CL of 1513ml/h/kg in BALB/c mice.The values for AUC and Cmax are 107.3μM and 296.7μM,respectively, in CD-1 mice.And the IC50 values are 58.4μM and 212.7μM,respectively, in BALB/c mice.The large volume of distribution are 322ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice.WHI-P97 (intraperitoneal injection;40mg/kg;24 days) prevents ovalbumin-sensitized mice the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion in mice. WHI-P97 inhibits the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion.

Animal Model:

BALB/c mouse model of allergic asthma

Dosage:

40mg/kg

Administration:

intraperitoneal injection;24 days

Result:

Showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels.

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

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摩尔浓度计算公式

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  • 计算结果

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    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):