Date published: 2026-5-2

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NPC1L1 Inhibitors

NPC1L1 inhibitors represents a diverse array of compounds that play a crucial role in regulating cholesterol absorption in the small intestine. Ezetimibe stands out as a direct inhibitor that binds to NPC1L1, significantly impeding its function in facilitating the absorption of cholesterol. By specifically targeting the molecular machinery responsible for cholesterol transport, Ezetimibe represents a potent tool in managing cholesterol levels by limiting its entry into the systemic circulation. This direct inhibition of NPC1L1 offers a targeted approach to modulate cholesterol homeostasis, showcasing the significance of understanding the intricate molecular interactions involved in lipid absorption. Complementing the direct inhibitors are various compounds that exert their inhibitory effects on NPC1L1 through indirect mechanisms. Lomitapide, an MTP inhibitor, reduces the availability of triglyceride-rich lipoproteins, substrates for cholesterol absorption via NPC1L1, showcasing the interconnectedness of lipid metabolism in regulating NPC1L1 function. Lovastatin, a well-known HMG-CoA reductase inhibitor, disrupts cholesterol synthesis, indirectly impacting NPC1L1 by lowering intracellular cholesterol levels. The intricate balance between endocytic processes and NPC1L1 function is evident in compounds like Imipramine and Genistein, which modulate endosomal trafficking and cholesterol trafficking, respectively. These indirect inhibitors underscore the complex interplay of cellular processes that regulate cholesterol absorption through NPC1L1. Collectively, NPC1L1 inhibitors provides a spectrum of strategies, from direct binding to disrupting related pathways, to effectively modulate cholesterol absorption.

Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Ezetimibe

163222-33-1sc-205690
sc-205690A
25 mg
100 mg
$96.00
$241.00
12
(2)

Ezetimibe inhibits NPC1L1 directly by preventing the absorption of cholesterol in the small intestine. It binds to NPC1L1, limiting its function in cholesterol transport, thereby reducing cholesterol absorption.

Imipramine

50-49-7sc-507545
5 mg
$190.00
(0)

Imipramine inhibits NPC1L1 indirectly by disrupting the endocytic pathway. By altering endosomal trafficking, imipramine can affect the transport and processing of NPC1L1, leading to reduced cholesterol absorption.

Lovastatin

75330-75-5sc-200850
sc-200850A
sc-200850B
5 mg
25 mg
100 mg
$29.00
$90.00
$339.00
12
(1)

Lovastatin inhibits HMG-CoA reductase, indirectly affecting NPC1L1 by reducing the synthesis of cholesterol. Lower intracellular cholesterol levels result in decreased substrate availability for NPC1L1-mediated absorption.

Amiodarone

1951-25-3sc-480089
5 g
$318.00
(1)

Amiodarone inhibits NPC1L1 indirectly by altering membrane lipid composition. This disrupts the organization of lipid rafts, impacting the proper localization and function of NPC1L1 in cholesterol absorption.

β-Sitosterol

83-46-5sc-204432
sc-204432A
10 g
25 g
$61.00
$217.00
5
(1)

Sitosterol competitively inhibits NPC1L1 by acting as a cholesterol analog. Its structural similarity to cholesterol allows it to interfere with the binding and absorption of cholesterol by NPC1L1 in the small intestine.

CHOLESTYRAMINE RESIN

11041-12-6sc-507509
5 g
$210.00
(0)

Cholestyramine inhibits NPC1L1 indirectly by binding to bile acids in the intestine. This interrupts the enterohepatic circulation of bile acids, leading to increased hepatic conversion of cholesterol to bile acids and reduced NPC1L1 activity.

Genistein

446-72-0sc-3515
sc-3515A
sc-3515B
sc-3515C
sc-3515D
sc-3515E
sc-3515F
100 mg
500 mg
1 g
5 g
10 g
25 g
100 g
$45.00
$164.00
$200.00
$402.00
$575.00
$981.00
$2031.00
46
(1)

Genistein inhibits NPC1L1 indirectly by modulating intracellular cholesterol trafficking. By influencing endocytic processes, genistein disrupts the proper localization and function of NPC1L1 in cholesterol absorption.

Berberine

2086-83-1sc-507337
250 mg
$92.00
1
(0)

Berberine inhibits NPC1L1 indirectly by reducing the expression of intestinal NPC1L1. Through transcriptional regulation, berberine decreases the levels of NPC1L1, leading to a subsequent reduction in cholesterol absorption.

Nonaethylene glycol monododecyl ether

3055-99-0sc-281106
sc-281106A
50 g
100 g
$184.00
$321.00
(1)

Nonaethylene glycol monododecyl ether inhibits NPC1L1 indirectly by disrupting lipid rafts in the intestinal membrane. This alteration in membrane composition interferes with the proper localization and function of NPC1L1, reducing cholesterol absorption.

Nifedipine

21829-25-4sc-3589
sc-3589A
1 g
5 g
$59.00
$173.00
15
(1)

Nifedipine inhibits NPC1L1 indirectly by modulating cellular calcium levels. By influencing calcium-dependent processes, nifedipine disrupts the proper localization and function of NPC1L1 in cholesterol absorption.