中文名称: MK-4256
英文名称: MK-4256
CAS No: 1104599-69-0
分子式: C27H23FN8O
分子量: 494.52
M11666 MK-4256 ≥98% (psaitong)
包装规格:
5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(≥100mg/mL)
产品描述:

基本信息

产品编号:

M11666

产品名称:

MK-4256

CAS:

1104599-69-0

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C27H23FN8O

溶于液体

-80℃

6个月

分子量:

494.52

-20℃

1个月

化学名: 

3-((1R,3R)-3-(5-(4-Fluorophenyl)-1H-imidazol-2-yl)-1-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-5-methyl-1,2,4-oxadiazole

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

2.0222mL

10.1108mL

20.2216mL

5mM

0.4044mL

2.0222mL

4.0443mL

10mM

0.2022mL

1.0111mL

2.0222mL

 

生物活性

产品描述

一种有效的选择性 SSTR3 拮抗剂。

靶点

IC50:0.66nM (human SSTR3),0.36nM (mouse SSTR3)

 

体外研究

MK-4256 has excellent selectivity against other SSTR subtypes based on in vitro assays.In human receptor binding assays,MK-4256 has IC50s>2μM for SSTR1 and SSTR2.Although the binding IC50 values on SSTR4 and SSTR5 are below 1μM,there is still >500-fold selectivity.MK-4256 is tested in functional antagonist assays against SSTR4 and SSTR5.The IC50 values are greater than 5μM (at least 5000-fold selectivity).MK-4256 inhibits radiolabeled MK-499 binding of the hERG channel with an IC50=1.74μM.In a functional patch clamp assay,MK-4256 exhibits 50% blockade of hERG at 3.4μM concentration.

体内研究

MK-4256 reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses as low as 0.03mg/kg po.MK-4256 demonstrates exceptional SSTR3-mediated glucose lowering efficacy in the mouse oGTT model with minimal hypoglycemia risk.MK-4256 achieves complete ablation of glucose excursion (109%) at 1 mg/kg po.MK-4256 reduces the glucose excursion from 0.003 to 10mg/kg in a dose-dependent manner.The plasma Cmax of MK-4256 is determined from parallel mouse PK studies. At 0.01,0.1,and 1mg/kg oral dose,MK-4256 achieves Cmax of 7,88,and 493nM,respectivley.

 

推荐实验方法(仅供参考)

动物实验:

 

Mice

To demonstrate that the observed glucose lowering by MK-4256 is SSTR3-dependent,the effect of a maximally efficacious dosage of MK-4256 on blood glucose excursion during an oGTT wasinvestigated in SSTR3 KO mice. Administration of MK4256 (1mg/kg) and compound A (1mg/kg;des-F-sitagliptin,a DPP-4 inhibitor included as a positive control) to agematched C57BL/6N male WT mice significantly inhibits blood glucose excursion by 112 and 91%,respectively. 

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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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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