MedKoo Cat#: 525676 | Name: MK-0916

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

MK-0916
MK-0916
CAS#633317-53-0

Theoretical Analysis

MedKoo Cat#: 525676

Name: MK-0916

CAS#: 633317-53-0

Chemical Formula: C18H19ClFN3

Exact Mass: 331.1252

Molecular Weight: 331.82

Elemental Analysis: C, 65.16; H, 5.77; Cl, 10.68; F, 5.73; N, 12.66

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
MK0916; MK 0916; MK-0916
IUPAC/Chemical Name
3-((1s,3s)-1-(4-chlorophenyl)-3-fluorocyclobutyl)-4,5-dicyclopropyl-4H-1,2,4-triazole
InChi Key
OGYZYOKAXYFLIU-UJKQEGAGSA-N
InChi Code
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/t14-,18+
SMILES Code
F[C@H]1C[C@](C2=NN=C(C3CC3)N2C4CC4)(C5=CC=C(Cl)C=C5)C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 331.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: 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.