MK-0916

• CAT Number: I008041
• CAS Number: 633317-53-0
• Molecular Formula: C18H19ClFN3
• Molecular Weight: 331.819
• Purity: ≥95%
• Target: Type 1 Inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: 3-[1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-1,2,4-triazole
• InChI: InChI=1S/C18H19ClFN3/c19-13-5-3-12(4-6-13)18(9-14(20)10-18)17-22-21-16(11-1-2-11)23(17)15-7-8-15/h3-6,11,14-15H,1-2,7-10H2
• InChIKey: OGYZYOKAXYFLIU-UHFFFAOYSA-N
• SMILES: C1CC1C2=NN=C(N2C3CC3)C4(CC(C4)F)C5=CC=C(C=C5)Cl

MK-0916 (Cat.No:I008041) 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.

Reference

1:Pharmacokinetic-pharmacodynamic studies of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor MK-0916 in healthy subjects. 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.Br J Clin Pharmacol. 2013 Dec;76(6):917-31. doi: 10.1111/bcp.12131. PMID: 23594227 Free PMC Article2:Efficacy and safety of the selective 11β-HSD-1 inhibitors MK-0736 and MK-0916 in overweight and obese patients with hypertension. Shah S, Hermanowski-Vosatka A, Gibson K, Ruck RA, Jia G, Zhang J, Hwang PM, Ryan NW, Langdon RB, Feig PU.J Am Soc Hypertens. 2011 May-Jun;5(3):166-76. doi: 10.1016/j.jash.2011.01.009. Epub 2011 Mar 21. PMID: 21419745 3:Effects of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor, MK-0916, in patients with type 2 diabetes mellitus and metabolic syndrome. Feig PU, Shah S, Hermanowski-Vosatka A, Plotkin D, Springer MS, Donahue S, Thach C, Klein EJ, Lai E, Kaufman KD.Diabetes Obes Metab. 2011 Jun;13(6):498-504. doi: 10.1111/j.1463-1326.2011.01375.x. PMID: 21272190