Date published: 2026-5-1

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BSEP Inhibitors

BSEP inhibitors constitute a distinctive chemical class characterized by their unique capability to interact with the Bile Salt Export Pump (BSEP), an integral protein localized within the hepatocyte cell membrane. These compounds modulate the function of BSEP, a vital component of the hepatobiliary transport system responsible for the efflux of bile salts into the bile canaliculus. By engaging with BSEP, these inhibitors can disrupt its normal function, thereby influencing the hepatobiliary transport of bile salts.

The significance of BSEP inhibitors lies in their ability to shed light on the intricate mechanisms governing hepatobiliary transport and bile salt homeostasis. Researchers have been actively investigating the precise molecular interactions between BSEP and these inhibitors, aiming to unravel the underlying molecular intricacies. This endeavor has led to the identification of diverse chemical structures within the BSEP inhibitor class, each possessing distinct molecular attributes that contribute to their binding affinity and impact on BSEP-mediated transport processes. The exploration of BSEP inhibitors not only advances our understanding of hepatic physiology but also holds broader implications for the intricate network of pathways involved in bile salt regulation. As researchers delve deeper into the mechanistic insights of BSEP inhibitors, they provide valuable contributions to the intricate puzzle of hepatobiliary transport, yielding insights into the intricate coordination of bile salt dynamics within the physiological context.

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Items 1 to 10 of 11 total

Display:

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Troglitazone

97322-87-7sc-200904
sc-200904B
sc-200904A
5 mg
10 mg
25 mg
$110.00
$204.00
$435.00
9
(1)

Interferes with BSEP function by altering membrane fluidity and disrupting its transport activity, potentially leading to cholestasis.

Bosentan

147536-97-8sc-210957
10 mg
$195.00
3
(1)

Inhibits BSEP by directly interacting with the transporter, resulting in decreased bile acid transport and potential hepatotoxicity.

Glyburide (Glibenclamide)

10238-21-8sc-200982
sc-200982A
sc-200982D
sc-200982B
sc-200982C
1 g
5 g
25 g
100 g
500 g
$46.00
$61.00
$117.00
$173.00
$530.00
36
(1)

Can inhibit BSEP function by modulating cellular signaling pathways or affecting membrane properties, contributing to bile acid retention.

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$97.00
$328.00
$676.00
$1467.00
6
(1)

Acts as a BSEP inhibitor by binding to the transporter and disrupting its function, potentially leading to liver injury.

Fluvastatin

93957-54-1sc-279169
50 mg
$250.00
(0)

May inhibit BSEP by altering membrane composition and affecting transporter function, potentially causing hepatobiliary adverse effects.

Ketoconazole

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

Inhibits BSEP by interfering with its function at the molecular level, which can lead to cholestasis and impaired bile acid secretion.

Erythromycin

114-07-8sc-204742
sc-204742A
sc-204742B
sc-204742C
5 g
25 g
100 g
1 kg
$57.00
$245.00
$831.00
$1331.00
4
(3)

Can inhibit BSEP by altering its function, potentially causing accumulation of bile acids and hepatotoxicity.

Naringenin

480-41-1sc-219338
25 g
$245.00
11
(1)

Acts on BSEP by modulating cellular pathways or directly interacting with the transporter, potentially affecting bile acid transport.

Tolvaptan

150683-30-0sc-364638
sc-364638A
10 mg
50 mg
$125.00
$624.00
(0)

May impact BSEP function through its effects on cellular processes, potentially leading to impaired bile acid secretion.

Lopinavir

192725-17-0sc-207831
10 mg
$132.00
6
(1)

Inhibits BSEP function by directly interacting with the transporter, potentially causing hepatotoxicity and alterations in bile acid transport.