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MK-6892

Catalog No. TQ0108   CAS 917910-45-3

MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).

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MK-6892 Chemical Structure
MK-6892, CAS 917910-45-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 115.00
5 mg In stock $ 247.00
10 mg In stock $ 356.00
25 mg In stock $ 596.00
50 mg In stock $ 839.00
100 mg In stock $ 1,160.00
500 mg In stock $ 2,320.00
1 mL * 10 mM (in DMSO) In stock $ 260.00
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Purity: 99.03%
Purity: 99.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
Targets&IC50 GPR109A:16 nM (EC50), GPR109A:4 nM (Ki)
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 [1].
Molecular Weight 386.4
Formula C19H22N4O5
CAS No. 917910-45-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (129.40 mM), sonification is recommended.

TargetMolReferences and Literature

1. Shen HC, et al. 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. J Med Chem. 2010 Mar 25;53(6):2666-70. 2. Kim HY, et al. Discovery of 4-(phenyl)thio-1H-pyrazole derivatives as agonists of GPR109A, a high affinity niacin receptor. Arch Pharm Res. 2015 Jun;38(6):1019-32.

TargetMolCitations

1. Zhu S, Yuan Q, Li X, et al.Molecular recognition of niacin and lipid-lowering drugs by the human hydroxycarboxylic acid receptor 2.Cell Reports.2023, 42(11).

Related compound libraries

This product is contained In the following compound libraries:
Endocrinology-Hormone Compound Library NO PAINS Compound Library Anti-Cancer Compound Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

MK-6892 917910-45-3 Endocrinology/Hormones GPCR/G Protein GPR HCAR2 PUMA-G HM74A HCA2 Inhibitor MK 6892 GPR109A inhibit MK6892 inhibitor

 

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