| Identification | Back Directory | [Name]
MK4256 | [CAS]
1104599-69-0 | [Synonyms]
MK4256
1H-Pyrido[3,4-b]indole, 3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1-(5-methyl-1,2,4-oxadiazol-3-yl)-1-(1-methyl-1H-pyrazol-4-yl)-, (1R,3R)- | [Molecular Formula]
C27H23FN8O | [MOL File]
1104599-69-0.mol | [Molecular Weight]
494.52 |
| Chemical Properties | Back Directory | [Boiling point ]
826.7±75.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 100 mg/mL (202.22 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
13.02±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
MK-4256 is a potent and selective SSTR3 antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively. | [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[1]. | [References]
[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. DOI:10.1021/ml300063m
[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. DOI:10.1021/ml500028c |
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InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
| Company Name: |
MedChemExpress
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021-58955995 |
| Website: |
www.medchemexpress.com |
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