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MK-4256  ≥98%

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包装规格：1mg 5mg 10mg 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℃

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