Date published: 2025-12-18

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GPR119 Activators

GPR119 activators encompass a variety of compounds that directly or indirectly enhance the activity of the GPR119 protein. Direct activators include bioactive lipids such as oleoylethanolamide (OEA), and synthetic small molecules like PSN632408, AR231453, MBX-2982, GSK1292263, and APD668. These compounds bind to the orthosteric site of GPR119, initiating a conformational change that triggers the adenylate cyclase-cAMP signaling pathway. This pathway plays a crucial role in modulating insulin secretion in response to glucose, a key process in glucose homeostasis.On the other hand, indirect activators operate by supplying the body with precursors that are metabolized into endogenous compounds that can bind and activate GPR119. Examples of these precursors are sodium oleate, sodium linoleate, sodium palmitate, sodium stearate, diacylglycerol, and palmitic acid. Once absorbed, these compounds can be metabolized to various N-acylethanolamines, including OEA, linoleoylethanolamide (LEA), palmitoylethanolamide (PEA), and stearoylethanolamide (SEA), all of which can bind to and activate GPR119. The activation of GPR119 leads to the initiation of the adenylate cyclase-cAMP pathway, which results in increased cAMP levels and enhanced insulin secretion, thereby contributing to glucose homeostasis.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Oleylethanolamide

111-58-0sc-201400
sc-201400A
10 mg
50 mg
$88.00
$190.00
1
(1)

OEA is a bioactive lipid that directly activates GPR119. It binds to the receptor's orthosteric site, triggering a conformational change that activates intracellular signaling cascades, including the adenylate cyclase-cAMP pathway.

PSN 375963 hydrochloride

388575-52-8sc-204219
sc-204219A
10 mg
50 mg
$175.00
$739.00
(0)

PSN 375963 hydrochloride functions as a GPR119 agonist, engaging in selective binding to the receptor's allosteric site. Its unique molecular architecture facilitates specific hydrophobic interactions and stabilizes receptor conformation, enhancing downstream signaling. The compound exhibits a favorable kinetic profile, characterized by a moderate binding affinity that allows for sustained receptor activation, thereby influencing metabolic pathways and cellular signaling dynamics effectively.

AS 1269574

330981-72-1sc-361109
sc-361109A
10 mg
50 mg
$155.00
$620.00
(0)

AS 1269574 acts as a GPR119 modulator, characterized by its ability to induce conformational changes in the receptor through unique electrostatic interactions. This compound's distinct structural features promote enhanced receptor dimerization, which is crucial for optimal signaling. Its reaction kinetics reveal a rapid onset of action, allowing for effective modulation of intracellular pathways. The compound's solubility profile further supports its dynamic interactions within biological systems.

2-Oleoylglycerol

3443-84-3sc-213888
sc-213888B
sc-213888A
1 mg
5 mg
10 mg
$52.00
$173.00
$316.00
2
(1)

2-Oleoylglycerol functions as a GPR119 agonist, exhibiting a unique affinity for the receptor that facilitates specific ligand-receptor interactions. Its hydrophobic tail enhances membrane integration, promoting receptor activation through allosteric modulation. The compound's kinetic profile indicates a sustained engagement with GPR119, leading to prolonged signaling effects. Additionally, its lipid-like properties contribute to its ability to traverse cellular membranes efficiently, influencing metabolic pathways.

Sodium oleate

143-19-1sc-215879
sc-215879A
250 mg
1 g
$45.00
$100.00
3
(1)

Sodium oleate, a salt of oleic acid, can be metabolized to OEA, which directly activates GPR119. This increases cAMP levels and leads to enhanced insulin secretion.

Linoleic Acid

60-33-3sc-200788
sc-200788A
sc-200788B
sc-200788C
100 mg
1 g
5 g
25 g
$33.00
$63.00
$163.00
$275.00
4
(2)

Sodium linoleate, a salt of linoleic acid, can be metabolized to linoleoylethanolamide (LEA), which can activate GPR119, leading to increased cAMP levels and enhanced insulin secretion.

Sodium palmitate

408-35-5sc-215881
sc-215881A
sc-215881B
sc-215881C
5 g
10 g
25 g
500 g
$105.00
$195.00
$260.00
$2100.00
6
(1)

Sodium palmitate, a salt of palmitic acid, can be metabolized to palmitoylethanolamide (PEA), which can activate GPR119, leading to increased cAMP levels and enhanced insulin secretion.

Sodium stearate

822-16-2sc-215884
sc-215884A
1 g
5 g
$41.00
$102.00
1
(0)

Sodium stearate, a salt of stearic acid, can be metabolized to stearoylethanolamide (SEA), which can activate GPR119, leading to increased cAMP levels and enhanced insulin secretion.

1,2-Dioctanoyl-sn-glycerol

60514-48-9sc-202397
sc-202397A
10 mg
50 mg
$46.00
$249.00
2
(1)

Diacylglycerol can be metabolized to various N-acylethanolamines that can activate GPR119, leading to increased cAMP levels and enhanced insulin secretion.

Palmitic Acid

57-10-3sc-203175
sc-203175A
25 g
100 g
$112.00
$280.00
2
(0)

Palmitic acid can be metabolized to palmitoylethanolamide (PEA), which can activate GPR119, leading to increased cAMP levels and enhanced insulin secretion.