Date published: 2026-3-3

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GPR30 Activators

GPR30, also known as G protein-coupled estrogen receptor 1 (GPER1), is a transmembrane receptor that belongs to the G protein-coupled receptor (GPCR) family. Its primary function involves mediating the rapid non-genomic effects of estrogen signaling in various tissues and cell types. GPR30 is widely expressed in multiple organs, including the brain, cardiovascular system, reproductive organs, and immune cells. Upon activation by estrogen, GPR30 initiates signaling cascades that modulate cellular processes such as cell proliferation, migration, survival, and gene expression, thereby influencing diverse physiological functions.The activation of GPR30 typically involves ligand binding, where estrogen acts as a potent agonist. Upon ligand binding, GPR30 undergoes conformational changes that allow it to interact with heterotrimeric G proteins, leading to the activation of downstream signaling pathways. One of the key pathways activated by GPR30 is the epidermal growth factor receptor (EGFR) transactivation pathway, which involves the rapid phosphorylation of EGFR and subsequent activation of intracellular signaling cascades such as the mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinase (PI3K) pathways. Additionally, GPR30 can also signal through other pathways, including cyclic adenosine monophosphate (cAMP) production, intracellular calcium mobilization, and activation of protein kinase B (Akt). Through these signaling mechanisms, GPR30 activation regulates various cellular responses, contributing to the physiological effects of estrogen in different tissues and organs.

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Genistein

446-72-0sc-3515
sc-3515A
sc-3515B
sc-3515C
sc-3515D
sc-3515E
sc-3515F
100 mg
500 mg
1 g
5 g
10 g
25 g
100 g
$45.00
$164.00
$200.00
$402.00
$575.00
$981.00
$2031.00
46
(1)

Genistein acts as a GPR30 ligand, engaging in selective receptor binding that initiates unique signaling cascades. Its isoflavonoid structure facilitates specific interactions with the receptor's binding site, promoting conformational changes that activate intracellular pathways. The compound's hydrophilic and hydrophobic balance enhances its interaction with lipid membranes, influencing receptor dynamics and modulating the kinetics of signal transduction in a nuanced manner.

Quercetin Dihydrate

6151-25-3sc-203225
sc-203225A
5 g
25 g
$36.00
$61.00
1
(1)

Quercetin Dihydrate functions as a GPR30 ligand, exhibiting a distinctive ability to modulate receptor activity through its flavonoid framework. This compound engages in specific hydrogen bonding and hydrophobic interactions with the receptor, leading to altered receptor conformation and downstream signaling. Its antioxidant properties may influence cellular redox states, further impacting receptor-mediated pathways and enhancing the complexity of signal modulation within various cellular environments.

β-Estradiol

50-28-2sc-204431
sc-204431A
500 mg
5 g
$63.00
$182.00
8
(1)

β-Estradiol acts as a GPR30 agonist, showcasing a unique capacity to influence receptor dynamics through its steroidal structure. It engages in specific hydrophobic interactions and forms critical van der Waals contacts with the receptor, facilitating conformational changes that activate distinct signaling cascades. This interaction can modulate intracellular calcium levels and influence gene expression, highlighting its role in diverse physiological processes and cellular responses.

Bisphenol A

80-05-7sc-391751
sc-391751A
100 mg
10 g
$300.00
$490.00
5
(0)

Bisphenol A, an industrial chemical, indirectly activates GPR30 by influencing estrogen receptor pathways. It binds to estrogen receptors, altering their activity and subsequently impacting GPR30 activation. This compound operates through a non-genomic mechanism, affecting rapid signaling cascades and ultimately promoting GPR30 activity.

Tamoxifen Citrate

54965-24-1sc-203288
100 mg
$83.00
12
(1)

Tamoxifen Citrate exhibits intriguing interactions with GPR30, characterized by its ability to stabilize receptor conformation through unique hydrogen bonding and hydrophobic interactions. This compound can induce allosteric modulation, altering receptor affinity for endogenous ligands. Its kinetic profile suggests a slow dissociation rate, allowing prolonged receptor engagement, which may lead to sustained signaling effects. This behavior underscores its potential to influence various cellular pathways and responses.

ICI 182,780

129453-61-8sc-203435
sc-203435A
1 mg
10 mg
$83.00
$187.00
34
(1)

ICI 182,780 is a selective GPR30 modulator that engages in distinctive molecular interactions, particularly through its capacity to form specific electrostatic and van der Waals forces with the receptor. This compound exhibits unique binding kinetics, characterized by a rapid association phase followed by a gradual dissociation, which enhances its receptor occupancy. Its structural properties facilitate conformational changes in GPR30, potentially influencing downstream signaling cascades and cellular responses.

Quercetin

117-39-5sc-206089
sc-206089A
sc-206089E
sc-206089C
sc-206089D
sc-206089B
100 mg
500 mg
100 g
250 g
1 kg
25 g
$11.00
$17.00
$110.00
$250.00
$936.00
$50.00
33
(2)

Quercetin acts as a GPR30 modulator, exhibiting unique binding characteristics that involve hydrophobic interactions and hydrogen bonding with the receptor. Its kinetic profile reveals a slow onset of action, allowing for sustained receptor engagement. This compound's structural flexibility enables it to induce specific conformational shifts in GPR30, which may alter signaling pathways and affect cellular behavior. Additionally, its antioxidant properties may influence receptor interactions indirectly.

Resveratrol

501-36-0sc-200808
sc-200808A
sc-200808B
100 mg
500 mg
5 g
$80.00
$220.00
$460.00
64
(2)

Resveratrol, a polyphenolic compound, indirectly activates GPR30 by modulating intracellular pathways. It enhances GPR30 activity through the AMP-activated protein kinase (AMPK) pathway. Resveratrol activates AMPK, leading to increased GPR30 expression and function. This compound's indirect activation of GPR30 highlights its role in integrating cellular energy status with GPR30 signaling, providing a unique avenue for modulating receptor activity.

Diethylstilbestrol

56-53-1sc-204720
sc-204720A
sc-204720B
sc-204720C
sc-204720D
1 g
5 g
25 g
50 g
100 g
$71.00
$287.00
$547.00
$1098.00
$2185.00
3
(1)

Diethylstilbestrol (DES), a synthetic estrogen, directly activates GPR30 by binding to its receptor site. This compound triggers GPR30-mediated signaling events, including the activation of the PI3K/Akt pathway. DES's direct activation of GPR30 highlights its estrogenic properties, making it a compound with specific effects on GPR30 receptor activation and downstream signaling cascades.

(S)-Equol

531-95-3sc-205502
sc-205502A
sc-205502B
sc-205502C
1 mg
5 mg
10 mg
25 mg
$34.00
$150.00
$260.00
$582.00
2
(2)

S-equol, a metabolite of daidzein, indirectly activates GPR30 by influencing estrogen receptor pathways. It binds to estrogen receptors, altering their activity and subsequently impacting GPR30 activation. This compound operates through a non-genomic mechanism, affecting rapid signaling cascades and ultimately promoting GPR30 activity. S-equol's indirect activation of GPR30 highlights its role in modulating estrogen signaling pathways.