1. GPCR/G Protein
  2. GPR109A
  3. MK-6892

MK-6892 

Cat. No.: HY-10680 Purity: 99.43%
Handling Instructions

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.

For research use only. We do not sell to patients.

MK-6892 Chemical Structure

MK-6892 Chemical Structure

CAS No. : 917910-45-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE MK-6892

    MK-6892 purchased from MCE. Usage Cited in: Glia. 2018 Feb;66(2):256-278.

    Representative images and quantitative analysis showing the effects of Niacin (1 mM, 10 min) and MK-6892 (10 lM, 10 min) on Akt phosphorylation levels in primary cultured microglia.
    • Biological Activity

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    • References

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    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.

    IC50 & Target

    Ki: 4 nM (GPR109A)[1]
    EC50: 16 nM (GPR109A)[1]

    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].

    Molecular Weight

    386.40

    Formula

    C₁₉H₂₂N₄O₅

    CAS No.

    917910-45-3

    SMILES

    OC(C=C1)=CN=C1C2=NOC(CC(C)(C)C(NC3=C(C(O)=O)CCCC3)=O)=N2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (129.40 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5880 mL 12.9400 mL 25.8799 mL
    5 mM 0.5176 mL 2.5880 mL 5.1760 mL
    10 mM 0.2588 mL 1.2940 mL 2.5880 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.43%

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    Keywords:

    MK-6892MK6892MK 6892GPR109AHM74APUMA-GHCA2HCAR2 Inhibitorinhibitorinhibit

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    Product Name:
    MK-6892
    Cat. No.:
    HY-10680
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