Date published: 2026-4-26

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RORα Inhibitors

RORα inhibitors function through various mechanisms to modulate the activity of RORα (Retinoic Acid Receptor-Related Orphan Receptor Alpha), a transcription factor integral to numerous physiological processes including circadian rhythm regulation, immune response, and metabolic homeostasis. A primary method of inhibiting RORα involves the use of inverse agonists or antagonists. These compounds bind directly to RORα, altering its conformation and thereby inhibiting its ability to regulate gene transcription. This direct interaction results in a diminished expression of genes under RORα's control, leading to significant impacts on processes regulated by this transcription factor, such as alterations in circadian rhythms, immune function, and lipid metabolism.

In addition to direct antagonism, another mechanism employed by RORα inhibitors is the modulation of signaling pathways and metabolic processes that are closely associated with RORα's function. These inhibitors can affect the cellular signaling environment, influencing the pathways that intersect with or regulate the activity of RORα. By altering these pathways, the inhibitors indirectly impact RORα's role in transcriptional regulation. This can lead to changes in cellular behaviors and processes where RORα plays a regulatory role, such as in inflammation, energy balance, and the body's circadian system. These diverse mechanisms of action employed by RORα inhibitors underscore the complex regulation of RORα activity and highlight the potential implications of modulating this transcription factor in various processes.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

SR 1001

1335106-03-0sc-507320
5 mg
$150.00
(0)

SR1001 is a synthetic compound that acts as an inverse agonist of RORα. It binds to RORα and inhibits its transcriptional activity, thereby reducing its regulatory effects on target genes.

12β-Hydroxydigitoxin

20830-75-5sc-213604
sc-213604A
1 g
5 g
$143.00
$694.00
(0)

12β-Hydroxydigitoxin, traditionally used for heart conditions, has been shown to inhibit RORα activity. It may indirectly inhibit RORα by interfering with its transcriptional regulation.

Melatonin

73-31-4sc-207848
sc-207848A
sc-207848B
sc-207848C
sc-207848D
sc-207848E
1 g
5 g
25 g
100 g
250 g
1 kg
$65.00
$73.00
$218.00
$697.00
$1196.00
$3574.00
16
(2)

Melatonin, a hormone regulating circadian rhythms, can modulate RORα activity. It may indirectly inhibit RORα by influencing circadian regulation and related gene expression.

Simvastatin

79902-63-9sc-200829
sc-200829A
sc-200829B
sc-200829C
50 mg
250 mg
1 g
5 g
$31.00
$89.00
$135.00
$443.00
13
(1)

Simvastatin, a cholesterol-lowering statin, has been reported to affect RORα activity. It might inhibit RORα by altering lipid metabolism pathways where RORα is involved.

Ketoconazole

65277-42-1sc-200496
sc-200496A
50 mg
500 mg
$63.00
$265.00
21
(1)

Ketoconazole, an antifungal agent, can influence various nuclear receptors. It may inhibit RORα by disrupting its role in regulating gene expression related to immune response and metabolism.

1,1-Dimethylbiguanide, Hydrochloride

1115-70-4sc-202000F
sc-202000A
sc-202000B
sc-202000C
sc-202000D
sc-202000E
sc-202000
10 mg
5 g
10 g
50 g
100 g
250 g
1 g
$20.00
$43.00
$63.00
$156.00
$260.00
$510.00
$31.00
37
(1)

1,1-Dimethylbiguanide, Hydrochloride, an antidiabetic drug, can affect AMPK pathways and potentially influence RORα signaling by altering the cellular energy status and metabolic pathways.

Pioglitazone

111025-46-8sc-202289
sc-202289A
1 mg
5 mg
$55.00
$125.00
13
(1)

Pioglitazone, a PPARγ agonist, might indirectly inhibit RORα through its effects on glucose metabolism and adipogenesis, pathways where RORα is implicated.

Chrysin

480-40-0sc-204686
1 g
$38.00
13
(1)

Chrysin, a flavonoid found in honey and propolis, has been reported to affect nuclear receptor activity. It could indirectly inhibit RORα by modulating its transcriptional regulation.

Sulfasalazine

599-79-1sc-204312
sc-204312A
sc-204312B
sc-204312C
1 g
2.5 g
5 g
10 g
$61.00
$77.00
$128.00
$209.00
8
(1)

Sulfasalazine, used in inflammatory bowel disease, can affect nuclear receptor activity. It might inhibit RORα by altering signaling pathways involved in inflammation and immune response.