| Name | MK-4256 |
| Description | MK-4256 is an effective and selective SSTR3 antagonist (IC50s: 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively). |
| In vitro | 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)[1]. MK-4256 inhibits radiolabeled MK-499 binding of the hERG channel (IC50=1.74 μM). MK-4256 has excellent selectivity against other SSTR subtypes based on in vitro assays and it also has IC50s >2 μM for SSTR1 and SSTR2, in human receptor binding assays. Although the binding IC50 values on SSTR4 and SSTR5 are below 1 μM, there is still >500-fold selectivity. MK-4256 exhibits 50% blockade of hERG at 3.4 μM concentration, in a functional patch-clamp assay[2]. |
| In vivo | MK-4256 decreases the glucose excursion from 0.003 to 10 mg/kg in a dose-dependent manner. MK-4256 decreases glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses of MK-4256 (0.03 mg/kg; p.o.) demonstrates exceptional SSTR3-mediated glucose-lowering efficacy in the mouse oGTT model with minimal hypoglycemia risk. MK-4256 (1 mg/kg; p.o.) achieves complete ablation of glucose excursion (109%). The plasma Cmax of MK-4256 is determined from parallel mouse PK studies. MK-4256 achieves Cmax of 7, 88, and 493 nM, respectively, at 0.01, 0.1, and 1 mg/kg oral dose [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (202.22 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 4 mg/mL (8.09 mM), Sonication is recommended.
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| Keywords | mouse SSTR3 | MK-4256 | MK4256 | MK 4256 | human SSTR3 |
| Inhibitors Related | 2-Aminoethanethiol | Octreotide Acetate | Octreotide | AGI-43192 | BIM-23190 aceate | Lanreotide acetate | L-797,591 hydrochloride | [Tyr3]Octreotate | L-796,778 | CYN 154806 TFA | Cortistatin-14 acetate | Somatostatin acetate |
United States
