Date published: 2025-11-1

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GPR3 Activators

GPR3 activators are a diverse set of chemical compounds known to selectively enhance the activity of the GPR3 protein, a member of the G protein-coupled receptor (GPCR) family. GPR3 is inherently involved in the regulation of cyclic adenosine monophosphate (cAMP) levels within the cell. As a constitutively active receptor, GPR3 maintains a basal level of cAMP, which is integral for various cellular functions, including signal transduction and the regulation of ion channels. Chemical activators of GPR3 typically work by binding to the receptor and stabilizing its active form, leading to an increase in cAMP production. This, in turn, activates protein kinase A (PKA), which then phosphorylates target proteins, thereby modulating cellular processes. Some activators might also influence the receptor's interaction with its G proteins, enhancing the signaling efficiency. The specificity of these activators is crucial, as they must preferentially target GPR3 without significantly affecting the broad family of GPCRs to ensure precise modulation of the signaling pathways.The mechanism of action for GPR3 activators is facilitated through their interaction with the receptor's ligand-binding domain, which is strategically positioned in the extracellular region of the protein. This interaction promotes a conformational change that propagates through the transmembrane domain, activating the G protein within the intracellular environment. The resulting signal cascade further perpetuates the cellular response to elevated cAMP levels, affecting various downstream targets that are critical for maintaining cellular homeostasis. GPR3 activators are structurally varied, allowing for selective binding and activation, and they can have different affinities for the receptor, which results in varied potency and efficacy. The activation of GPR3 by these chemical compounds is an intricate process that can integrate multiple signaling pathways to regulate physiological functions. The chemical entities that serve as activators for GPR3 are instrumental in understanding the receptor's role in cellular signaling and provide valuable insights into the modulation of cAMP-dependent pathways.

Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

D-erythro-Sphingosine-1-phosphate

26993-30-6sc-201383
sc-201383D
sc-201383A
sc-201383B
sc-201383C
1 mg
2 mg
5 mg
10 mg
25 mg
$162.00
$316.00
$559.00
$889.00
$1693.00
7
(1)

D-erythro-Sphingosine-1-phosphate functions as a GPR3 ligand, exhibiting selective binding affinity that triggers distinct intracellular signaling pathways. Its unique structural conformation allows for specific interactions with receptor domains, influencing downstream effects on cellular processes. The compound's hydrophobic regions enhance membrane permeability, while its phosphate group contributes to ionic interactions, modulating receptor activation and signaling kinetics in a targeted manner.

Forskolin

66575-29-9sc-3562
sc-3562A
sc-3562B
sc-3562C
sc-3562D
5 mg
50 mg
1 g
2 g
5 g
$76.00
$150.00
$725.00
$1385.00
$2050.00
73
(3)

Forskolin directly stimulates adenylyl cyclase, increasing intracellular levels of cAMP. As GPR3 is a G protein-coupled receptor that modulates cAMP production, forskolin's activation of adenylyl cyclase would indirectly enhance GPR3 signaling by increasing its primary second messenger, cAMP.

Isoproterenol Hydrochloride

51-30-9sc-202188
sc-202188A
100 mg
500 mg
$27.00
$37.00
5
(0)

Isoproterenol is a synthetic catecholamine that activates beta-adrenergic receptors, which can lead to increased cAMP production through Gs protein stimulation. This elevation in cAMP may enhance GPR3-associated signaling pathways, indirectly increasing GPR3 activity.

Rolipram

61413-54-5sc-3563
sc-3563A
5 mg
50 mg
$75.00
$212.00
18
(1)

Rolipram is a selective phosphodiesterase-4 inhibitor, leading to the accumulation of cAMP in the cell. Increased intracellular cAMP levels can potentiate GPR3 signaling due to GPR3's involvement in cAMP-mediated signal transduction.

IBMX

28822-58-4sc-201188
sc-201188B
sc-201188A
200 mg
500 mg
1 g
$159.00
$315.00
$598.00
34
(1)

IBMX is a non-selective inhibitor of phosphodiesterases, enzymes that degrade cAMP. By preventing cAMP breakdown, IBMX can indirectly enhance GPR3 activity by maintaining elevated cAMP levels, which play a crucial role in GPR3's signaling pathway.

PGE1 (Prostaglandin E1)

745-65-3sc-201223
sc-201223A
1 mg
10 mg
$30.00
$142.00
16
(4)

PGE1 activates G protein-coupled E-prostanoid receptors which can lead to increased cAMP production. This rise in cAMP may indirectly enhance GPR3 signaling, given GPR3s role in cAMP-mediated pathways.

Salbutamol

18559-94-9sc-253527
sc-253527A
25 mg
50 mg
$92.00
$138.00
(1)

Salbutamol is a beta-2 adrenergic agonist that elevates cAMP levels through the activation of Gs protein-coupled receptors. The resultant increase in cAMP can enhance GPR3 activity since GPR3 is implicated in cAMP-dependent signaling.

Anagrelide

68475-42-3sc-491875
25 mg
$147.00
(0)

Anagrelide inhibits phosphodiesterase 3, resulting in an increase in cAMP levels within the cell. This increase in cAMP can indirectly enhance the signaling of GPR3, a receptor that operates through cAMP-dependent pathways.

BAY 60-6583

910487-58-0sc-503262
10 mg
$210.00
(0)

BAY 60-6583 is an adenosine A2B receptor agonist that leads to increased intracellular cAMP. Through this mechanism, it can indirectly enhance GPR3 activity by augmenting the cAMP signaling pathway, which is central to GPR3 function.

Zardaverine

101975-10-4sc-201208
sc-201208A
5 mg
25 mg
$88.00
$379.00
1
(0)

Zardaverine is a dual-selective inhibitor of phosphodiesterase 3 and 4, leading to increased levels of cAMP. This elevation can indirectly potentiate GPR3 signaling due to the receptor's reliance on cAMP for its activity.