| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
MK-8245 (MK8245; MK 8245) is a novel and potent liver-targeted inhibitor of stearoyl-CoA desaturase (SCD) with anti-diabetic and anti-dyslipidemic activities. It inhibits stearoyl-CoA desaturase with an IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. It exhibits high anti-diabetic and anti-dyslipidemic efficacy in vivo and a significantly improved therapeutic window.
| ln Vitro |
MK-8245 is an effective SCD inhibitor that is liver-specific[1]. With IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1, MK-8245 has comparable potencies against SCD1 in humans, rats, and mice[1]. In the rat hepatocyte assay, where organic anion transporting polypeptides (OATPs) are functional and active with an IC50 of 68 nM, MK-8245 shows a considerable reduction of SCD. In the HepG2 cell assay, on the other hand, OATPs are only weakly active and have an IC50 of approximately 1 μM, indicating a lack of activity[1].
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| ln Vivo |
In rats, dogs, and rhesus monkeys, MK-8245 (10 mg/kg; po) has a tissue distribution profile that is concentrated in the liver and has little exposure in tissues linked to possible adverse events[1]. When given to eDIO mice before to the glucose challenge, MK-8245 increases glucose clearance in a dose-dependent manner[1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL6 mice, male SD (Sprague-Dawley) rats[1]
Doses: 10mg/kg Route of Administration: Oral administration Experimental Results: Exhibits a tissue distribution profile concentrated in the liver. |
| References | |
| Additional Infomation |
MK-8245 has been used in trials studying the treatment of Type 2 Diabetes Mellitus.
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| Molecular Formula |
C17H16N6O4FBR
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|---|---|
| Molecular Weight |
467.24914
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| Exact Mass |
466.04
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| CAS # |
1030612-90-8
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| Related CAS # |
MK-8245 Trifluoroacetate;1415559-41-9
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| PubChem CID |
24988881
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
698.3±65.0 °C at 760 mmHg
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| Flash Point |
376.1±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.737
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| LogP |
1.12
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
572
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UDXUBDGJHLPKFJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14BrFN6O2/c16-11-2-1-9(17)7-12(11)24-10-3-5-23(6-4-10)14-8-13(25-20-14)15-18-21-22-19-15/h1-2,7-8,10H,3-6H2,(H,18,19,21,22)
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| Chemical Name |
2-[5-[3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid
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| Synonyms |
MK-8245; MK 8245; MK8245; 4-(2-Bromo-5-fluorophenoxy)-1-[5-(2H-tetrazol-5-yl)-3-isoxazolyl]piperidine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% CMC+0.5% Tween-80: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1402 mL | 10.7009 mL | 21.4018 mL | |
| 5 mM | 0.4280 mL | 2.1402 mL | 4.2804 mL | |
| 10 mM | 0.2140 mL | 1.0701 mL | 2.1402 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00972322 | Completed Has Results | Drug: MK-8245 Drug: Comparator: placebo |
Type 2 Diabetes Mellitus | Merck Sharp & Dohme LLC | August 24, 2009 | Phase 1 |
| NCT00846391 | Terminated Has Results | Drug: MK8245 5 mg (twice a day) b.i.d. Drug: MK8245 50 mg b.i.d. |
Type 2 Diabetes Mellitus | Merck Sharp & Dohme LLC | December 2008 | Phase 2 |
| NCT00790556 | Completed Has Results | Drug: MK8245 Drug: Comparator: Placebo |
Type 2 Diabetes | Merck Sharp & Dohme LLC | October 2008 | Phase 1 |
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