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。

MK-4256 is a potent and selective SSTR3 antagonist with IC 50 s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.

Solid

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

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. He S, et al. The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2012 May 7;3(6):484-9.
[2]. He S, et al. Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.

In Vitro: DMSO : ≥ 100 mg/mL (202.22 mM)配制储备液