Date published: 2025-12-12

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megalin Activators

Megalin, a multifunctional endocytic receptor predominantly expressed in renal proximal tubule cells, plays a crucial role in the reabsorption of filtered proteins. The identified chemicals presented here, albeit not proven direct activators, modulate megalin activity through intricate cellular pathways. Gossypol, a natural compound, indirectly activates megalin by impacting the PI3K/AKT pathway, which regulates megalin expression and function in specific cellular contexts. Resveratrol, a polyphenol, indirectly activates megalin through its influence on SIRT1 activity, affecting pathways linked to megalin expression and trafficking. Sulforaphane, found in cruciferous vegetables, activates NRF2, indirectly promoting megalin expression by modulating cellular redox status and enhancing endocytic capacity. AICAR, an AMPK activator, indirectly activates megalin by modulating AMPK-dependent pathways, impacting megalin expression and trafficking in response to altered energy status.

Troglitazone, a PPARγ agonist, indirectly activates megalin by influencing PPARγ-dependent pathways, altering megalin expression and function transcriptionally. Raloxifene, a selective estrogen receptor modulator, indirectly activates megalin by modulating estrogen receptor signaling, impacting megalin expression and function in a hormone-dependent manner. Dasatinib, a tyrosine kinase inhibitor, indirectly activates megalin through its effects on Src family kinases, influencing megalin expression and function kinase-dependently. Parthenolide, found in feverfew, indirectly activates megalin by modulating NF-κB signaling, impacting megalin expression and function through altered transcriptional regulation. GW501516, a PPARδ agonist, indirectly activates megalin by influencing PPARδ-dependent pathways, altering megalin expression and function transcriptionally. Betulinic acid, a natural compound, indirectly activates megalin through its effects on the STAT3 pathway, influencing megalin expression and function transcriptionally. C646, a p300/CBP inhibitor, indirectly activates megalin by affecting histone acetylation, influencing megalin expression and function epigenetically. In conclusion, while direct megalin activators remain elusive, these chemicals show promise in influencing megalin activity through intricate cellular pathways, providing a foundation for further exploration into their regulatory roles in megalin-mediated endocytosis.

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Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Gossypol

303-45-7sc-200501
sc-200501A
25 mg
100 mg
$114.00
$225.00
12
(1)

Gossypol, a natural compound, affects the PI3K/AKT pathway. By modulating this pathway, gossypol indirectly activates megalin, as PI3K/AKT signaling plays a role in regulating megalin expression and function in certain cellular contexts, enhancing its endocytic activity.

Resveratrol

501-36-0sc-200808
sc-200808A
sc-200808B
100 mg
500 mg
5 g
$60.00
$185.00
$365.00
64
(2)

Resveratrol, a polyphenol, influences SIRT1 activity. Its impact on SIRT1 can indirectly activate megalin by affecting cellular pathways linked to megalin expression and trafficking, ultimately enhancing endocytic processes through modulation of intracellular signaling.

D,L-Sulforaphane

4478-93-7sc-207495A
sc-207495B
sc-207495C
sc-207495
sc-207495E
sc-207495D
5 mg
10 mg
25 mg
1 g
10 g
250 mg
$150.00
$286.00
$479.00
$1299.00
$8299.00
$915.00
22
(1)

Sulforaphane, found in cruciferous vegetables, activates NRF2. Through NRF2 activation, sulforaphane indirectly promotes megalin expression by modulating cellular redox status, resulting in enhanced endocytic capacity through NRF2-mediated regulation of megalin-related pathways.

AICAR

2627-69-2sc-200659
sc-200659A
sc-200659B
50 mg
250 mg
1 g
$60.00
$270.00
$350.00
48
(2)

AICAR, an AMPK activator, influences AMPK-dependent pathways. Indirectly, AICAR can activate megalin by modulating AMPK-related cellular processes, impacting megalin expression and trafficking, thereby enhancing endocytic activity in response to altered energy status.

Troglitazone

97322-87-7sc-200904
sc-200904B
sc-200904A
5 mg
10 mg
25 mg
$108.00
$200.00
$426.00
9
(1)

Troglitazone, a PPARγ agonist, affects PPARγ-dependent pathways. Indirectly, troglitazone can activate megalin by modulating PPARγ-related cellular processes, influencing megalin expression and function, leading to enhanced endocytic capacity through altered transcriptional regulation.

Raloxifene

84449-90-1sc-476458
1 g
$802.00
3
(0)

Raloxifene, a selective estrogen receptor modulator, influences estrogen receptor signaling. Indirectly, raloxifene can activate megalin by modulating estrogen receptor-dependent pathways, impacting megalin expression and function, leading to enhanced endocytic processes.

Dasatinib

302962-49-8sc-358114
sc-358114A
25 mg
1 g
$47.00
$145.00
51
(1)

Dasatinib, a tyrosine kinase inhibitor, affects Src family kinases. Indirectly, dasatinib can activate megalin by modulating Src kinase-dependent pathways, influencing megalin expression and function, leading to enhanced endocytic capacity through altered kinase activity.

Parthenolide

20554-84-1sc-3523
sc-3523A
50 mg
250 mg
$79.00
$300.00
32
(2)

Parthenolide, found in feverfew, affects NF-κB signaling. Indirectly, parthenolide can activate megalin by modulating NF-κB-dependent pathways, impacting megalin expression and function, leading to enhanced endocytic capacity through altered transcriptional regulation.

GW501516

317318-70-0sc-202642
sc-202642A
1 mg
5 mg
$80.00
$175.00
28
(3)

GW501516, a PPARδ agonist, influences PPARδ-dependent pathways. Indirectly, GW501516 can activate megalin by modulating PPARδ-related cellular processes, impacting megalin expression and function, leading to enhanced endocytic capacity through altered transcriptional regulation.

Betulinic Acid

472-15-1sc-200132
sc-200132A
25 mg
100 mg
$115.00
$337.00
3
(1)

Betulinic acid, a natural compound, affects the STAT3 pathway. Indirectly, betulinic acid can activate megalin by modulating STAT3-dependent pathways, influencing megalin expression and function, leading to enhanced endocytic capacity through altered transcriptional regulation.