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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1104599-69-0
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3808.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1600.0 |
| 规格： | 5 mg | 产品价格： | ￥3500.0 |
| 规格： | 10 mg | 产品价格： | ￥6000.0 |
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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 Cmax of MK-4256 is determined from parallel mouse PK studies. At 0.01, 0.1, and 1 mg/kg oral dose, MK-4256 achieves Cmax of 7, 88, and 493 nM, respectivley.
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with diabetes mellitus: a meta-analysis of randomised controlled trials. Lancet,2009,373:1765-1772. ［12］ American Diabetes Association. Diagnosis and classification of diabetes mellitus. Diabetes Care,2010,33 Suppl 1:S62-69. ［13］ World Health
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