Date published: 2025-10-25

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Oatp2 Inhibitors

Oatp2 inhibitors are a class of chemical compounds specifically designed to target and inhibit the function of Organic Anion Transporting Polypeptide 2 (Oatp2), a member of the solute carrier organic anion transporter family. Oatp2, also known as SLCO1B1, is primarily expressed in the liver and plays a critical role in the uptake of a wide range of endogenous and exogenous organic anions, including bile acids, hormones, and various drugs, from the bloodstream into hepatocytes. This transporter facilitates the hepatic clearance of these compounds by mediating their entry into liver cells, where they can be metabolized and excreted into the bile. Oatp2 is essential for maintaining the body's homeostasis by regulating the levels of various anionic substances in the circulation and ensuring their proper disposal or recycling. By inhibiting Oatp2, researchers can disrupt these transport processes, providing a powerful tool to study the specific roles of Oatp2 in hepatic function and systemic homeostasis.

In research settings, Oatp2 inhibitors are valuable for exploring the mechanisms of organic anion transport and the broader implications of Oatp2 function on liver metabolism and overall physiological regulation. By blocking Oatp2 activity, scientists can investigate how the inhibition affects the hepatic uptake and clearance of various substrates, particularly focusing on the impact on bile acid recycling, hormone levels, and the disposition of endogenous metabolites. This inhibition allows researchers to study the downstream effects on liver function, such as alterations in bile formation, lipid metabolism, and detoxification processes, and how these changes influence systemic homeostasis. Additionally, Oatp2 inhibitors provide insights into the interactions between Oatp2 and other transporters and enzymes involved in the hepatic clearance pathways, shedding light on the complex networks that regulate the movement of organic anions within the body. Through these studies, the use of Oatp2 inhibitors enhances our understanding of the critical role of transporters in liver physiology, the regulation of organic anion levels, and the broader implications of transporter activity on metabolic and detoxification processes.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$95.00
$322.00
$663.00
$1438.00
6
(1)

Rifampicin is a known inhibitor of OATP1B1, affecting the hepatic uptake of various substrates.

Cyclosporin A

59865-13-3sc-3503
sc-3503-CW
sc-3503A
sc-3503B
sc-3503C
sc-3503D
100 mg
100 mg
500 mg
10 g
25 g
100 g
$62.00
$90.00
$299.00
$475.00
$1015.00
$2099.00
69
(5)

Cyclosporine A inhibits OATP1B1, impacting the transport of endogenous and exogenous compounds.

Gemfibrozil

25812-30-0sc-204764
sc-204764A
5 g
25 g
$65.00
$262.00
2
(2)

Gemfibrozil and its glucuronide metabolite inhibit OATP1B1, potentially affecting drug pharmacokinetics.

Erythromycin

114-07-8sc-204742
sc-204742A
sc-204742B
sc-204742C
5 g
25 g
100 g
1 kg
$56.00
$240.00
$815.00
$1305.00
4
(3)

Erythromycin has been shown to interact with OATP1B1, affecting the transport of certain drugs.

Troglitazone

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

Troglitazone inhibits OATP1B1, which can influence the hepatic uptake of various compounds.

Nateglinide

105816-04-4sc-394067
sc-394067A
10 mg
25 mg
$188.00
$260.00
(0)

Nateglinide is both a substrate and inhibitor of OATP1B1, affecting its transport function.

Repaglinide

135062-02-1sc-219959
sc-219959A
sc-219959B
100 mg
250 mg
1 g
$215.00
$414.00
$1331.00
3
(0)

Repaglinide interacts with OATP1B1 and can inhibit its transport activity.

Losartan

114798-26-4sc-353662
100 mg
$127.00
18
(1)

Losartan, an angiotensin II receptor antagonist, is a substrate of OATP1B1 and can be affected by its inhibitors.

(+)-Irinotecan

97682-44-5sc-269253
10 mg
$61.00
1
(1)

Irinotecan, is influenced by OATP1B1 in terms of its hepatic uptake and clearance.

Glyburide (Glibenclamide)

10238-21-8sc-200982
sc-200982A
sc-200982D
sc-200982B
sc-200982C
1 g
5 g
25 g
100 g
500 g
$45.00
$60.00
$115.00
$170.00
$520.00
36
(1)

Glibenclamide is an OATP1B1 substrate; its transport can be affected by OATP1B1 inhibitors.