MK-6892Highly potential GPR109A agonist CAS# 917910-45-3 |
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| Cas No. | 917910-45-3 | SDF | Download SDF |
| PubChem ID | 15987030 | Appearance | Powder |
| Formula | C19H22N4O5 | M.Wt | 386.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (129.40 mM; Need ultrasonic) | ||
| Chemical Name | 2-[[2,2-dimethyl-3-[(3E)-3-(5-oxopyridin-2-ylidene)-1,2,4-oxadiazol-5-yl]propanoyl]amino]cyclohexene-1-carboxylic acid | ||
| SMILES | CC(C)(CC1=NC(=C2C=CC(=O)C=N2)NO1)C(=O)NC3=C(CCCC3)C(=O)O | ||
| Standard InChIKey | PHGMXUSKLSOOBC-JQIJEIRASA-N | ||
| Standard InChI | InChI=1S/C19H22N4O5/c1-19(2,18(27)21-13-6-4-3-5-12(13)17(25)26)9-15-22-16(23-28-15)14-8-7-11(24)10-20-14/h7-8,10,23H,3-6,9H2,1-2H3,(H,21,27)(H,25,26)/b16-14+ | ||
| 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-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.In Vitro:MK-6892 evokes a potent internalization of GPR109A in U2OS β-arrestin2-RrGFP cells.MK-6892 shows an EC50 value of 74 nM on calcium mobilization assay[2].In Vivo:MK-6892 is orally administered to WT or nicotinic acid (NA) receptor null mice on the same C57Bl/6 genetic background. After 15 min of 100 mg/kg dosing of MK-6892 to fed WT or NA receptor null mice, the blood levels of MK-6892 at 15 min are 229 μM (~950-fold greater than the in vitro EC50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148 μM (~620-fold greater than the in vitro EC50) in NA receptor null mice. MK-6892 effectively suppresses plasma FFA in the WT but not in the NA receptor null animals, indicating that the FFA reduction of MK-6892 is NA receptor-dependent. MK-6892 is selected for the studies because of its good PK and activity profiles in these two species (EC50=4.6 μM in the GTPγS assay for the rat NA receptor and 1.3 μM in the GTPγS assay for the dog NA receptor). Despite the significant weaker activity of MK-6892 in rat and dog with respect to that in human, MK-6892 shows good activity in reducing FFA in rat and dog models[1]. References: | |||||
MK-6892 Dilution Calculator
MK-6892 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.588 mL | 12.94 mL | 25.8799 mL | 51.7598 mL | 64.6998 mL |
| 5 mM | 0.5176 mL | 2.588 mL | 5.176 mL | 10.352 mL | 12.94 mL |
| 10 mM | 0.2588 mL | 1.294 mL | 2.588 mL | 5.176 mL | 6.47 mL |
| 50 mM | 0.0518 mL | 0.2588 mL | 0.5176 mL | 1.0352 mL | 1.294 mL |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.5176 mL | 0.647 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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Description: IC50 Value: 4.0 nM (Ki for Human GPR109A) [1] MK-6892 is a highly potential GPR109A agonists. in vitro: . Despite the increased serum shift of these compounds, the representative 1e was highly potent. Furthermore, these compounds had no activity on GPR109B and GPR81, the two most closely related GPCRs with ?96% and 50% sequence identity to GPR109A,respectively [1]. in vivo: NA or MK-6892 was orally administered to WT or NA receptor null mice on the same C57Bl/6 genetic background. After 15 min of 100 mpk dosing of NA or MK-6892 to fed WT or NA receptor null mice, the blood levels of MK-6892 at 15 min were 229 μM (?950-fold greater than the in vitro EC50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148 μM (?620-fold greater than the in vitro EC50) in NA receptor null mice [1]. Clinical trial: N/A
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Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.[Pubmed:20184326]
J Med Chem. 2010 Mar 25;53(6):2666-70.
Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR109A) agonists. Compound 1e (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good ancillary pharmacology, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
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