Date published: 2026-3-3

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ORMDL1 Activators

ORMDL1 activators are a class of chemical compounds that specifically enhance the functional activity of ORMDL1, a protein integral to sphingolipid metabolism. These activators function through various mechanisms that converge on the regulation and maintenance of sphingolipid homeostasis within the cell. For instance, sphingosine-1-phosphate (S1P) is a key activator that binds to its receptors, triggering signaling pathways such as PI3K/Akt and MAPK/ERK that are crucial for cell survival and proliferation. This activation can upregulate ORMDL1, given its role in sphingolipid metabolism, thereby enhancing its function. Compounds like ceramide and fingolimod also play significant roles; ceramide directly influences sphingolipid levels, prompting the cell to enhance ORMDL1 activity in response, while fingolimod-phosphate, an active metabolite of fingolimod, modulates S1P receptors, similarly affecting ORMDL1's regulatory function.

Additional activators include molecules that interact with various aspects of cellular metabolism and signal transduction pathways that are linked to ORMDL1. For example, brefeldin A disrupts the Golgi apparatus, indirectly causing an upregulation of ORMDL1 activity as the cell attempts to compensate for the disruption in sphingolipid processing. Myriocin, a serine palmitoyltransferase inhibitor, leads to a compensatory increase in ORMDL1 function to maintain sphingolipid synthesis. Statins like simvastatin, by inhibiting cholesterol synthesis, inadvertently affect sphingolipid metabolism, implicating ORMDL1 in the process of restoring lipid balance.

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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
$165.00
$322.00
$570.00
$907.00
$1727.00
7
(1)

S1P is a bioactive lipid that enhances the ORMDL1 function by binding to S1P receptors, which can lead to the activation of downstream signaling pathways such as PI3K/Akt or MAPK/ERK, both of which are involved in cellular survival and proliferation. Activation of these pathways can enhance ORMDL1 activity as it is involved in sphingolipid metabolism regulation.

C-8 Ceramide

74713-59-0sc-205233
sc-205233A
sc-205233B
1 mg
5 mg
25 mg
$19.00
$63.00
$228.00
1
(0)

Ceramide participates in sphingolipid metabolism and can influence the activity of ORMDL1, which is involved in this pathway. By altering the balance of ceramide levels, homeostatic mechanisms can enhance the function of ORMDL1 to regulate this balance within the cell.

FTY720

162359-56-0sc-202161
sc-202161A
sc-202161B
1 mg
5 mg
25 mg
$33.00
$77.00
$120.00
14
(1)

Fingolimod is phosphorylated in vivo to form fingolimod-phosphate, which acts as a sphingosine-1-phosphate receptor modulator. This interaction can enhance the ORMDL1 function by modulating the sphingolipid signaling pathway, which ORMDL1 is directly involved in.

Diazoxide

364-98-7sc-200980
1 g
$300.00
5
(1)

Diazoxide opens ATP-sensitive potassium channels, which leads to membrane hyperpolarization. This hyperpolarization can enhance calcium influx in certain cell types, and since calcium signaling can influence sphingolipid metabolism, it can indirectly enhance the ORMDL1 function.

Brefeldin A

20350-15-6sc-200861C
sc-200861
sc-200861A
sc-200861B
1 mg
5 mg
25 mg
100 mg
$31.00
$53.00
$124.00
$374.00
25
(3)

Brefeldin A disrupts the Golgi apparatus, where sphingolipid metabolism occurs. By disrupting this process, it can lead to compensatory mechanisms that enhance the activity of ORMDL1 as the cell attempts to restore homeostasis in sphingolipid metabolism.

Myriocin (ISP-1)

35891-70-4sc-201397
10 mg
$150.00
8
(2)

Myriocin is a potent inhibitor of serine palmitoyltransferase, the initial step in sphingolipid synthesis. Inhibition of this step can lead to upregulation of downstream enzymes and regulators such as ORMDL1 to compensate for the disrupted sphingolipid synthesis.

Progesterone

57-83-0sc-296138A
sc-296138
sc-296138B
1 g
5 g
50 g
$20.00
$52.00
$298.00
3
(1)

Progesterone interacts with its nuclear receptors, leading to transcriptional activation of genes involved in lipid metabolism. This can enhance the function of ORMDL1, as it regulates sphingolipid metabolism and thus its activity is enhanced in the presence of increased lipid synthesis.

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 inhibits HMG-CoA reductase, a key enzyme in cholesterol synthesis. As cholesterol and sphingolipid metabolism are interconnected, inhibition of cholesterol synthesis can enhance the functional activity of ORMDL1 in sphingolipid homeostasis.

GW4869

6823-69-4sc-218578
sc-218578A
5 mg
25 mg
$203.00
$611.00
24
(3)

GW4869 is a non-competitive inhibitor of neutral sphingomyelinase (nSMase), leading to reduced ceramide production from sphingomyelin. The resulting alteration in sphingolipid metabolism can enhance the function of ORMDL1 in maintaining sphingolipid equilibrium.

C2 Ceramide

3102-57-6sc-201375
sc-201375A
5 mg
25 mg
$124.00
$460.00
12
(1)

C2-ceramide is a cell-permeable ceramide analog that can influence sphingolipid metabolism. By increasing intracellular levels of ceramide, C2-ceramide can enhance the function of ORMDL1 as it regulates the balance of sphingolipids within the cell.