MK-0916

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

MedKoo CAT#: 525676

CAS#: 633317-53-0

Description: 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

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MK-0916
CAS# 633317-53-0
Instruction

Theoretical Analysis

MedKoo Cat#: 525676
Name: MK-0916
CAS#: 633317-53-0
Chemical Formula: C18H19ClFN3
Exact Mass: 331.13
Molecular Weight: 331.819
Elemental Analysis: C, 65.16; H, 5.77; Cl, 10.68; F, 5.73; N, 12.66

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.