Date published: 2025-10-11

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GPR101 Activators

GPR101 is an orphan G protein-coupled receptor (GPCR), meaning its endogenous ligand and physiological role are not well-defined. This receptor is predominantly expressed in the pituitary gland and the hypothalamus, regions of the brain that are critical for hormonal regulation and homeostasis. GPR101 has garnered significant interest due to its genetic association with X-linked acrogigantism (X-LAG), a condition characterized by excessive growth due to the overproduction of growth hormone.

The GPR101 gene is located on the X chromosome, and duplications in this gene are strongly linked to the development of X-LAG, suggesting that GPR101 overexpression leads to abnormal growth hormone secretion. This has led to the hypothesis that GPR101 may be involved in the signaling pathways that regulate pituitary function and growth hormone release.Despite its association with pathological growth, the normal physiological function of GPR101 remains elusive. It is speculated to be involved in neuroendocrine signaling given its expression profile. The receptor's activity and regulation could be influenced by various factors including hormones, intracellular messengers, and pharmacological agents, which may modulate its expression or activity.

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Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

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 activates adenylate cyclase, increasing cAMP levels, which can modulate GPCR expression.

PMA

16561-29-8sc-3576
sc-3576A
sc-3576B
sc-3576C
sc-3576D
1 mg
5 mg
10 mg
25 mg
100 mg
$40.00
$129.00
$210.00
$490.00
$929.00
119
(6)

PMA activates protein kinase C, which can influence GPCR gene transcription.

Retinoic Acid, all trans

302-79-4sc-200898
sc-200898A
sc-200898B
sc-200898C
500 mg
5 g
10 g
100 g
$65.00
$319.00
$575.00
$998.00
28
(1)

Retinoic acid regulates gene expression and may affect GPCR expression during differentiation.

5-Azacytidine

320-67-2sc-221003
500 mg
$280.00
4
(1)

A DNA methyltransferase inhibitor that can demethylate DNA and potentially upregulate gene expression.

Trichostatin A

58880-19-6sc-3511
sc-3511A
sc-3511B
sc-3511C
sc-3511D
1 mg
5 mg
10 mg
25 mg
50 mg
$149.00
$470.00
$620.00
$1199.00
$2090.00
33
(3)

An HDAC inhibitor that can change chromatin structure and increase gene expression.

Sodium Butyrate

156-54-7sc-202341
sc-202341B
sc-202341A
sc-202341C
250 mg
5 g
25 g
500 g
$30.00
$46.00
$82.00
$218.00
19
(3)

Another HDAC inhibitor that can lead to hyperacetylation of histones and affect gene expression.

Lithium

7439-93-2sc-252954
50 g
$214.00
(0)

Lithium can modulate GSK-3 activity, influencing Wnt signaling and possibly GPCR expression.

Valproic Acid

99-66-1sc-213144
10 g
$85.00
9
(1)

Valproic acid is an HDAC inhibitor that can alter gene expression, potentially affecting GPR101.

β-Estradiol

50-28-2sc-204431
sc-204431A
500 mg
5 g
$62.00
$178.00
8
(1)

As a steroid hormone, estradiol can regulate gene expression through estrogen receptor-mediated signaling.

Dexamethasone

50-02-2sc-29059
sc-29059B
sc-29059A
100 mg
1 g
5 g
$76.00
$82.00
$367.00
36
(1)

A glucocorticoid that can modulate gene expression, including that of GPCRs.