| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
MK-6892 (MK6892) is a novel, potent and selective full agonist for GPR109A, which is a high affinity nicotinic acid receptor. GPR109A is activated with Ki and GTPγS EC50 values of 4 nM and 16 nM on Human GPR109A, respectively. Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR109A) agonists. In rats and dogs, MK-6892 showed superior therapeutic window over niacin with respect to FFA reduction versus vasodilation, along with good ancillary pharmacology, good PK across species, and exceptionally clean off-target profiles.
| Targets |
GPR109A ( Ki = 4 nM ); GPR109A ( EC50 = 16 nM )
|
|---|---|
| ln Vitro |
MK-6892 stimulates GPR109A to internalize powerfully in U2OS β-arrestin2-RrGFP cells.In the calcium mobilization assay, MK-6892 exhibits an EC50 value of 74 nM[2].
|
| ln Vivo |
MK-6892 is given orally to mice bearing the same genetic background (C57Bl/6) that are WT or nicotinic acid (NA) receptor null. The blood levels of MK-6892 at 15 minutes 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. This is after feeding WT or NA receptor null mice 100 mg/kg of MK-6892 for 15 minutes. MK-6892 efficiently reduces plasma FFA in WT animals but not in NA receptor null animals, suggesting that MK-6892's FFA reduction is dependent on NA receptors. MK-6892 has been chosen for the research due to its favorable PK and activity profiles in these two species (EC50= 1.3 μM for the dog NA receptor and 4.6 μM for the rat NA receptor in the GTPηS assay). Although MK-6892 exhibits significantly less activity in rat and dog models compared to human models, it still demonstrates good activity in reducing FFA in these models[1].
|
| References |
|
| Molecular Formula |
C19H22N4O5
|
|---|---|
| Molecular Weight |
386.408
|
| Exact Mass |
386.16
|
| Elemental Analysis |
C, 59.06; H, 5.74; N, 14.50; O, 20.70
|
| CAS # |
917910-45-3
|
| Appearance |
Solid powder
|
| SMILES |
CC(C)(CC1=NC(=NO1)C2=NC=C(C=C2)O)C(=O)NC3=C(CCCC3)C(=O)O
|
| InChi Key |
CJHXBFSJXDUJHP-UHFFFAOYSA-N
|
| InChi Code |
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/h7-8,10,24H,3-6,9H2,1-2H3,(H,21,27)(H,25,26)
|
| Chemical Name |
2-[[3-[3-(5-hydroxypyridin-2-yl)-1,2,4-oxadiazol-5-yl]-2,2-dimethylpropanoyl]amino]cyclohexene-1-carboxylic acid
|
| Synonyms |
MK-6892; MK 6892; MK6892
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~129.4 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 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 (6.47 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 (6.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5879 mL | 12.9396 mL | 25.8792 mL | |
| 5 mM | 0.5176 mL | 2.5879 mL | 5.1758 mL | |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5879 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA