MK-4256 - CAS:1104599-69-0 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	MK-4256
英文名称:	MK-4256
别名:	3-((1R,3R)-3-(5-(4-氟苯基)-1H-咪唑-2-基)-1-(1-甲基-1H-吡唑-4-基)-2,3,4,9-四氢-1H-吡啶并[3,4-b]吲哚-1-基)-5-甲基-1,2,4-恶二唑 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
CAS No:	1104599-69-0	分子式:	C₂₇H₂₃FN₈O	分子量:	494.52
CAS No:	1104599-69-0
分子式:	C₂₇H₂₃FN₈O
分子量:	494.52

点击下载产品说明书(PDF)

M11666 MK-4256 ≥98% (psaitong)

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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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