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Chemical Structure : MK-4256
Catalog No.: PC-61088Not For Human Use, Lab Use Only.
MK-4256 is a potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.
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MK-4256 is a potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.
MK-4256 reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po, with minimal hypoglycemia risk.
Preclinical tirals of MK-4256 are discontinued due to dose-dependent QTc in conscious cardiovascular (CV) dog model.
| M.Wt | 494.534 | |
| Formula | C27H23FN8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. He S, et al. ACS Med Chem Lett. 2012 May 7;3(6):484-9.
2. He S, et al. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.
3. He S, et al. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535.
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