CAS NO: | 633317-53-0 |
包装: | 50mg, 100mg, 250mg |
规格: | ≥98% |
MK-0916 is an 11β-hydroxysteroid dehydrogenase type 1 inhibitor used for patients with type 2 diabetes mellitus and metabolic syndrome and obesity-related disorders. MK-0916 produces mechanism-based activation of the hypothalamic-pituitary-adrenal axis, resulting in mean increases in adrenal androgen levels that remains within the normal range. References: Harno E, Cottrell EC, Yu A, DeSchoolmeester J, Gutierrez PM, Denn M, Swales JG, Goldberg FW, Bohlooly-Y M, Andersén H, Wild MJ, Turnbull AV, Leighton B, White A. 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms. Endocrinology. 2013 Dec;154(12):4580-93. doi: 10.1210/en.2013-1613. Epub 2013 Oct 29. PubMed PMID: 24169553; PubMed Central PMCID: PMC4192288. 2: Wright DH, Stone JA, Crumley TM, Wenning L, Zheng W, Yan K, Yang AY, Sun L, Cilissen C, Ramael S, Hermanowski-Vosatka A, Langdon RB, Gottesdiener KM, Wagner JA, Lai E. Pharmacokinetic-pharmacodynamic studies of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor MK-0916 in healthy subjects. Br J Clin Pharmacol. 2013 Dec;76(6):917-31. doi: 10.1111/bcp.12131. PubMed PMID: 23594227; PubMed Central PMCID: PMC3845315. 3: Anagnostis P, Katsiki N, Adamidou F, Athyros VG, Karagiannis A, Kita M, Mikhailidis DP. 11beta-Hydroxysteroid dehydrogenase type 1 inhibitors: novel agents for the treatment of metabolic syndrome and obesity-related disorders? Metabolism. 2013 Jan;62(1):21-33. doi: 10.1016/j.metabol.2012.05.002. Epub 2012 May 30. Review. PubMed PMID: 22652056. 4: Shah S, Hermanowski-Vosatka A, Gibson K, Ruck RA, Jia G, Zhang J, Hwang PM, Ryan NW, Langdon RB, Feig PU. Efficacy and safety of the selective 11β-HSD-1 inhibitors MK-0736 and MK-0916 in overweight and obese patients with hypertension. J Am Soc Hypertens. 2011 May-Jun;5(3):166-76. doi: 10.1016/j.jash.2011.01.009. Epub 2011 Mar 21. PubMed PMID: 21419745. 5: Feig PU, Shah S, Hermanowski-Vosatka A, Plotkin D, Springer MS, Donahue S, Thach C, Klein EJ, Lai E, Kaufman KD. Effects of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor, MK-0916, in patients with type 2 diabetes mellitus and metabolic syndrome. Diabetes Obes Metab. 2011 Jun;13(6):498-504. doi: 10.1111/j.1463-1326.2011.01375.x. PubMed PMID: 21272190.
纯度:≥98%
CAS:633317-53-0