MK-8245SCD inhibitor,potent and liver-selective CAS# 1030612-90-8 |
- A939572
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- MK-8245 Trifluoroacetate
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Quality Control & MSDS
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| Cas No. | 1030612-90-8 | SDF | Download SDF |
| PubChem ID | 24988881 | Appearance | Powder |
| Formula | C17H16BrFN6O4 | M.Wt | 467.25 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 19 mg/mL (40.66 mM; Need ultrasonic and warming) | ||
| Chemical Name | 2-[5-[3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid | ||
| SMILES | C1CN(CCC1OC2=C(C=CC(=C2)F)Br)C3=NOC(=C3)C4=NN(N=N4)CC(=O)O | ||
| Standard InChIKey | UJEAABFSXKCSGI-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 values of 1 nM, 3 nM and 3 nM for human, rat and mouse SCD1. | |||||
| Targets | SCD1 (human) | SCD1 (rat) | SCD1 (mouse) | |||
| IC50 | 1 nM | 3 nM | 3 nM | |||
MK-8245 Dilution Calculator
MK-8245 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1402 mL | 10.7009 mL | 21.4018 mL | 42.8036 mL | 53.5045 mL |
| 5 mM | 0.428 mL | 2.1402 mL | 4.2804 mL | 8.5607 mL | 10.7009 mL |
| 10 mM | 0.214 mL | 1.0701 mL | 2.1402 mL | 4.2804 mL | 5.3505 mL |
| 50 mM | 0.0428 mL | 0.214 mL | 0.428 mL | 0.8561 mL | 1.0701 mL |
| 100 mM | 0.0214 mL | 0.107 mL | 0.214 mL | 0.428 mL | 0.535 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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MK-8245 is a potent and liver-selective inhibitor of stearoyl-CoA desaturase (SCD) with IC50 value of 1nM [1].
SCD1 represents a therapeutic target for the treatment of type II diabetes, dyslipidemia, obesity, and metabolic diseases. As an inhibitor of SCD1, MK-8245 shows potency in both the rat enzyme and hepatocyte assay. There are no significant differences in potencies between the rat, mouse, and human SCD1. MK-8245 is developed as a liver-targeting SCD inhibitor. It demonstrates a liver-targeted tissue distribution profile resulting from a substrate recognition by organic anionic transporter proteins (OATPs) [1, 2].
MK-8245 is effective at lowering glucose level. It can improve glucose clearance dose-dependently with ED50 value of 7mg/kg. In the chronic eDIO mouse study, MK-8245 shows prevention of body weight gain with the maximally efficacious dose of 20 mg/kg bid based on body weight and liver triglyceride reduction [1].
References:
[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.
[2] Lachance N, Guiral S, Huang Z, Leclerc JP, Li CS, Oballa RM, Ramtohul YK, Wang H, Wu J, Zhang L. Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series. Bioorg Med Chem Lett. 2012 Jan 1;22(1):623-7.
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Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.[Pubmed:21661758]
J Med Chem. 2011 Jul 28;54(14):5082-96.
The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia has been limited by preclinical adverse events associated with inhibition of SCD in skin and eye tissues. To establish a therapeutic window, we embarked on designing liver-targeted SCD inhibitors by utilizing molecular recognition by liver-specific organic anion transporting polypeptides (OATPs). In doing so, we set out to target the SCD inhibitor to the organ believed to be responsible for the therapeutic efficacy (liver) while minimizing its exposure in the tissues associated with mechanism-based SCD depletion of essential lubricating lipids (skin and eye). These efforts led to the discovery of MK-8245 (7), a potent, liver-targeted SCD inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window.
