ABC-A1 Activators
ABC-A1 Activators are a collection of chemical compounds that augment the functional activity of ABC-A1 through various signaling pathways, primarily by upregulating its expression or enhancing its lipid transport capacity. T0901317 and GW3965 are powerful LXR agonists that stimulate the transcription of the ABCA1 gene by directly engaging with the LXR response elements in the gene promoter, leading to increased ABC-A1 activity in cholesterol efflux. Similarly, endogenous ligands like 22(R)-hydroxycholesterol and synthetic compoundslike 9-cis-retinoic acid enhance ABC-A1 function by acting on nuclear receptors (LXR and RXR respectively) that regulate ABCA1 gene expression, promoting ABC-A1's role in lipid transport. Statins such as Rosuvastatin indirectly upregulate ABCA1 gene expression via inhibition of HMG-CoA reductase, which lowers intracellular cholesterol and triggers a homeostatic response to activate ABC-A1. Sulfosuccinimidyl oleate and cholesteryl hemisuccinate act as lipid analogs, upregulating LXR target genes, including ABCA1, and enhancing ABC-A1 activity in cholesterol efflux mechanisms. Additionally, 4-Phenylbutyrate, through histone deacetylase inhibition, and dexamethasone, via glucocorticoid response elements, indirectly promote ABC-A1 expression, contributing to improved lipid transport functionality.
Quercetin, a flavonoid, is thought to increase ABC-A1 expression by influencing transcription factor activity, while Pioglitazone, a PPARγ agonist, augments ABC-A1 activity indirectly by upregulating LXR, which in turn activates ABC-A1 transcription. The complex interplay of these activators, through their targeted effects on nuclear receptor signaling, transcriptional regulation, and cholesterol metabolism, collectively enhance the functional activity of ABC-A1. This underscores the intricate network of pathways that converge on the regulation of ABC-A1, each activator contributing to the overall efficacy of ABC-A1 in maintaining cellular lipid homeostasis and preventing cholesterol accumulation by facilitating its transport out of cells.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
T 0901317 | 293754-55-9 | sc-202824 sc-202824A | 10 mg 50 mg | $89.00 $224.00 | 5 | |
T0901317 is a potent and selective agonist of the liver X receptor (LXR), which regulates the expression of ABC-A1 by binding to LXR response elements in the ABCA1 gene promoter region, leading to the transcriptional activation of ABC-A1, increasing its protein levels and functional activity in cholesterol efflux. | ||||||
GW3965 | 405911-09-3 | sc-490151 sc-490151A sc-490151B | 10 mg 50 mg 1 g | $260.00 $872.00 $1637.00 | ||
GW3965 is another selective LXR agonist that enhances ABC-A1 activity by a similar mechanism as T0901317, stimulating the transcription of the ABCA1 gene and thereby increasing the functional output of ABC-A1 in transporting lipids across cell membranes. | ||||||
22(R)-hydroxycholesterol | 17954-98-2 | sc-205106 sc-205106A sc-205106B | 1 mg 5 mg 10 mg | $110.00 $357.00 $612.00 | 1 | |
22(R)-hydroxycholesterol is an oxysterol that serves as an endogenous LXR ligand. By activating LXR, it upregulates ABC-A1 expression, enhancing its role in mediating cholesterol and phospholipid efflux from cells. | ||||||
9-cis-Retinoic acid | 5300-03-8 | sc-205589 sc-205589B sc-205589C sc-205589D sc-205589A | 1 mg 25 mg 250 mg 500 mg 5 mg | $71.00 $424.00 $3121.00 $5722.00 $148.00 | 10 | |
9-cis-retinoic acid is a retinoid that acts as an agonist for the retinoid X receptor (RXR), which forms heterodimers with LXR. This dimerization is necessary for the transcriptional activation of LXR-target genes, including ABCA1, thus promoting ABC-A1-mediated lipid transport. | ||||||
Rosuvastatin | 287714-41-4 | sc-481834 | 10 mg | $145.00 | 8 | |
Rosuvastatin is a statin that indirectly activates ABC-A1 by inhibiting HMG-CoA reductase, leading to upregulation of ABCA1 gene expression through a compensatory mechanism aimed at reducing intracellular cholesterol levels. | ||||||
Sodium phenylbutyrate | 1716-12-7 | sc-200652 sc-200652A sc-200652B sc-200652C sc-200652D | 1 g 10 g 100 g 1 kg 10 kg | $77.00 $166.00 $622.00 $5004.00 $32783.00 | 43 | |
4-Phenylbutyrate is a histone deacetylase inhibitor that can indirectly increase ABC-A1 expression by promoting a more open chromatin structure, thereby allowing transcription factors like LXR to more easily access the ABCA1 promoter. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $91.00 $139.00 $374.00 | 36 | |
Dexamethasone is a glucocorticoid that can increase ABC-A1 expression through glucocorticoid response elements in the ABCA1 gene promoter, thus indirectly enhancing ABC-A1-mediated lipid efflux. | ||||||
Pioglitazone | 111025-46-8 | sc-202289 sc-202289A | 1 mg 5 mg | $55.00 $125.00 | 13 | |
Pioglitazone is a PPARγ agonist that indirectly enhances ABC-A1 activity by upregulating LXR, as PPARγ activation can lead to an increase in LXR expression, subsequently activating ABC-A1 transcription and function. | ||||||
Quercetin | 117-39-5 | sc-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 | |
Quercetin is a flavonoid that has been shown to increase ABC-A1 expression potentially by modulating transcription factor activity or through its antioxidant properties, which may influence the pathways that regulate ABCA1 gene expression and activity. | ||||||