MK-8245 | CAS#1030612-90-8 | 1415559-41-9 | SCD inhibitor

MedKoo Cat#: 525705 | Name: MK-8245

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Description:

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

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

MK-8245

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

Theoretical Analysis

MedKoo Cat#: 525705

Name: MK-8245

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

Chemical Formula: C17H16BrFN6O4

Exact Mass:

Molecular Weight: 467.26

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 150.00
25mg	USD 250.00
50mg	USD 450.00
100mg	USD 650.00
200mg	USD 950.00
500mg	USD 1,650.00
1g	USD 2,850.00
2g	USD 4,650.00
5g	USD 7,250.00

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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

View handling instruction

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/

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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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, SÃ¸rensen 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.