MK-8245
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525705

CAS#: 1030612-90-8 (free base);

Description: MK-8245 is a potent, liver-targeted SCD inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window. MK-8245 was believed to inhibit the SCD enzyme solely in the liver and not in other tissues for the following reasons. When SCD inhibition has been measured by desaturation index in tissues of rodents treated with MK-8245, the desaturation index was significantly reduced in liver but not in other tissues such as skin, eye and adipose tissue.

Chemical Structure

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MK-8245
CAS# 1030612-90-8 (free base);
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525705
Name: MK-8245
CAS#: 1030612-90-8 (free base);
Chemical Formula: C17H16BrFN6O4
Exact Mass: 0.00
Molecular Weight: 467.255
Elemental Analysis: C, 43.70; H, 3.45; Br, 17.10; F, 4.07; N, 17.99; O, 13.70

Price and Availability

Size Price Availability Quantity
10mg USD 150
25mg USD 250
50mg USD 450
100mg USD 650
200mg USD 950
500mg USD 1650
1g USD 2850
2g USD 4650
5g USD 7250
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Related CAS #: 1415559-41-9 (TFA)  

Synonym: MK-8245; MK8245; MK8245

IUPAC/Chemical Name: 2-(5-(3-(4-(2-bromo-5-fluorophenoxy)piperidin-1-yl)isoxazol-5-yl)-2H-tetrazol-2-yl)acetic acid

InChi Key: UJEAABFSXKCSGI-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H16BrFN6O4/c18-12-2-1-10(19)7-13(12)28-11-3-5-24(6-4-11)15-8-14(29-22-15)17-20-23-25(21-17)9-16(26)27/h1-2,7-8,11H,3-6,9H2,(H,26,27)

SMILES Code: O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O

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 soluble in water.

Shelf Life: >5 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: MK-8245, a liver-targeted SCD inhibitor believed to inhibit the SCD enzyme solely in the liver and not in other tissues for the following reasons. When SCD inhibition has been measured by desaturation index in tissues of rodents treated with MK-8245, the desaturation index was significantly reduced in liver but not in other tissues such as skin, eye and adipose tissue.        

Product Data:
Product Data
Instruction:
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Biological target: MK-8245 is a potent, liver-targeted SCD inhibitor.
In vitro activity: MK8245 was evaluated using recombinant HCV culture systems. Considering current HCV treatments, to avoid the emergence of direct anti-viral agents-resistant viruses, combination therapy with direct anti-viral agents and host-targeted agents would be optimal. With this viewpoint, this study confirmed MK8245's additive or synergistic anti-HCV effects on current direct anti-viral agents and interferon-alpha therapy. Reference: Antiviral Res. 2016 Aug;132:262-7. https://pubmed.ncbi.nlm.nih.gov/27392483/
In vivo activity: These studies reveal novel Ras-dependent functions of Wnt signaling in remodeling the lipid metabolism of cancerous hepatocytes in zebrafish and identify the SCD inhibitor MK8245 as a candidate drug for therapeutic intervention. Reference: Cancer Res. 2018 Oct 1;78(19):5548-5560. https://pubmed.ncbi.nlm.nih.gov/30065049/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 74.3 159.09
DMSO:PBS (pH 7.2) (1:1) 0.5 1.07

Preparing Stock Solutions

The following data is based on the product molecular weight 467.26 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: 1. Nio Y, Hasegawa H, Okamura H, Miyayama Y, Akahori Y, Hijikata M. Liver-specific mono-unsaturated fatty acid synthase-1 inhibitor for anti-hepatitis C treatment. Antiviral Res. 2016 Aug;132:262-7. doi: 10.1016/j.antiviral.2016.07.003. Epub 2016 Jul 5. PMID: 27392483. 2. Yao Y, Sun S, Wang J, Fei F, Dong Z, Ke AW, He R, Wang L, Zhang L, Ji MB, Li Q, Yu M, Shi GM, Fan J, Gong Z, Wang X. Canonical Wnt Signaling Remodels Lipid Metabolism in Zebrafish Hepatocytes following Ras Oncogenic Insult. Cancer Res. 2018 Oct 1;78(19):5548-5560. doi: 10.1158/0008-5472.CAN-17-3964. Epub 2018 Jul 31. PMID: 30065049. 3. Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96. doi: 10.1021/jm200319u. Epub 2011 Jun 28. PMID: 21661758.
In vitro protocol: 1. Nio Y, Hasegawa H, Okamura H, Miyayama Y, Akahori Y, Hijikata M. Liver-specific mono-unsaturated fatty acid synthase-1 inhibitor for anti-hepatitis C treatment. Antiviral Res. 2016 Aug;132:262-7. doi: 10.1016/j.antiviral.2016.07.003. Epub 2016 Jul 5. PMID: 27392483.
In vivo protocol: 1. Yao Y, Sun S, Wang J, Fei F, Dong Z, Ke AW, He R, Wang L, Zhang L, Ji MB, Li Q, Yu M, Shi GM, Fan J, Gong Z, Wang X. Canonical Wnt Signaling Remodels Lipid Metabolism in Zebrafish Hepatocytes following Ras Oncogenic Insult. Cancer Res. 2018 Oct 1;78(19):5548-5560. doi: 10.1158/0008-5472.CAN-17-3964. Epub 2018 Jul 31. PMID: 30065049. 2. Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96. doi: 10.1021/jm200319u. Epub 2011 Jun 28. PMID: 21661758.

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1: Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28. PubMed PMID: 21661758.