Date published: 2025-11-2

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GPR40 Activators

GPR40 activators belong to a specific chemical class of compounds that are known for their ability to interact with and activate the G-protein coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1). GPR40 is primarily expressed in pancreatic beta cells and certain tissues in the gastrointestinal tract, making it a key player in the regulation of glucose and lipid metabolism. These activators are characterized by their unique structural properties that allow them to bind to the receptor and initiate intracellular signaling cascades. When GPR40 is activated by these compounds, it triggers a series of events within the cell that ultimately leads to the release of insulin and the modulation of glucose and lipid homeostasis.Chemically, GPR40 activators encompass a diverse group of molecules, with some of the most well-known belonging to the class of long-chain free fatty acids, such as palmitic acid and oleic acid. These compounds are typically characterized by their hydrophobic nature, with a long hydrocarbon tail and a carboxylic acid functional group at one end. The specific binding mechanism of GPR40 activators involves their interaction with a well-defined binding pocket on the receptor's surface. This interaction leads to a conformational change in the receptor, allowing it to activate intracellular signaling pathways, including the Gq/11 protein pathway, leading to calcium mobilization and insulin secretion.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

GW 9508

885101-89-3sc-203069
10 mg
$125.00
(0)

GW 9508 is a potent agonist of GPR40, characterized by its ability to engage in hydrophobic interactions with specific residues in the receptor's transmembrane domains. This binding stabilizes the receptor in an active conformation, promoting enhanced signaling through the phospholipase C pathway. The compound's unique steric properties facilitate a rapid onset of action, influencing receptor dynamics and potentially modulating downstream metabolic processes. Its selectivity underscores its role in fine-tuning cellular responses.

TUG-424

1082058-99-8sc-222379
sc-222379A
5 mg
25 mg
$278.00
$909.00
(0)

TUG-424 acts as a selective agonist for GPR40, exhibiting unique binding characteristics that enhance receptor activation. Its molecular structure allows for specific hydrogen bonding with key amino acids, promoting a conformational shift that amplifies intracellular signaling cascades. The compound's kinetic profile indicates a swift interaction with the receptor, leading to a pronounced effect on lipid metabolism. Additionally, TUG-424's distinct hydrophobic regions contribute to its receptor affinity and specificity.

4-Hydroxy-isophthalic acid dimethyl ester

5985-24-0sc-336445
1 g
$144.00
(0)

4-Hydroxy-isophthalic acid dimethyl ester serves as a potent GPR40 modulator, characterized by its ability to engage in specific hydrophobic and electrostatic interactions with the receptor. This compound facilitates a unique allosteric modulation, enhancing receptor sensitivity to endogenous ligands. Its structural features promote efficient receptor dimerization, influencing downstream signaling pathways. The compound's rapid binding kinetics and favorable solubility profile further optimize its interaction dynamics with GPR40.

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)

As a polyunsaturated fatty acid, linoleic acid can activate GPR40, potentially boosting its expression.

Docosa-4Z,7Z,10Z,13Z,16Z,19Z-hexaenoic Acid (22:6, n-3)

6217-54-5sc-200768
sc-200768A
sc-200768B
sc-200768C
sc-200768D
100 mg
1 g
10 g
50 g
100 g
$92.00
$206.00
$1744.00
$7864.00
$16330.00
11
(1)

DHA is an omega-3 fatty acid that may act on GPR40 to induce its expression and affect insulin secretion.

α-Linolenic Acid

463-40-1sc-205545
sc-205545A
50 mg
250 mg
$37.00
$113.00
2
(2)

This plant-based omega-3 fatty acid can modulate GPR40 expression by acting as an endogenous ligand.

Oleic Acid

112-80-1sc-200797C
sc-200797
sc-200797A
sc-200797B
1 g
10 g
100 g
250 g
$36.00
$102.00
$569.00
$1173.00
10
(1)

Oleic acid, a monounsaturated fat, could increase GPR40 expression due to its role as a natural agonist.

Palmitic Acid

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

Palmitic acid is a saturated fatty acid that may influence GPR40 expression through its agonistic activity.

MEDICA 16

87272-20-6sc-203131
sc-203131A
5 mg
10 mg
$188.00
$260.00
1
(1)

Medica 16 is a synthetic ligand for GPR40 that may increase its expression, influencing insulin dynamics.