MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

MK-4256

CAS No. : 1104599-69-0

MCE 国际站：MK-4256

产品活性：MK-4256 是一种有效的选择性 SSTR3 拮抗剂。在人和小鼠受体结合测定中，IC₅₀ 分别为 0.66 nM 和 0.36 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Somatostatin Receptor

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

In Vivo: MK-4256 reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses as low as 0.03 mg/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 10 mg/kg in a dose-dependent manner. The plasma C_max of MK-4256 is determined from parallel mouse PK studies. At 0.01, 0.1, and 1 mg/kg oral dose, MK-4256 achieves C_max of 7, 88, and 493 nM, respectivley.

相关产品：Bioactive Compound Library Plus  |  Somatostatin-28 (sheep)  |  BIM-23190  |  sst2 Receptor agonist-1  |  Cortistatin 14, human, rat  |  Pasireotide (diaspartate)  |  Octreotide pamoate  |  PRL 2915  |  CYN 154806  |  BIM-23056 TFA  |  MAT2A-IN-1  |  L-797591  |  TT-232  |  DOTA-NOC  |  SSTR4 agonist 3  |  SSTR5 antagonist 2  |  Cortistatin-14 TFA  |  J-2156 TFA  |  Cyclosomatostatin TFA  |  L-803087  |  Veldoreotide  |  Angiopeptin TFA  |  [Nle8] Somatostatin (1-28)  |  MAT2A-IN-3  |  Somatostatin-28 (1-14)

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

货号: HY-13466

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。