Date published: 2025-10-25

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Oatp3 Inhibitors

OATP3 inhibitors belong to a distinctive chemical class that plays a crucial role in modulating the activity of the Organic Anion Transporting Polypeptide 3 (OATP3) transporters. OATP3 is a type of membrane protein found primarily in the cells of various tissues, especially in the liver and the kidney. Its main function is to facilitate the translocation of endogenous and exogenous compounds across cellular membranes. OATP3, as a member of the Solute Carrier Organic Anion Transporter (SLCO) family, specifically focuses on the uptake of anionic substrates, which encompass a wide array of molecules such as bile acids, hormones, and various drugs. Inhibitors of OATP3 are characterized by their capacity to hinder or reduce the transport function of OATP3 proteins. These inhibitors are typically designed to competitively bind to the substrate-binding site of the OATP3 transporter, thus impeding the uptake of specific substrates. By obstructing the transmembrane transport of various molecules, OATP3 inhibitors can have significant implications for cellular homeostasis and systemic drug distribution. Their mechanism of action centers around altering the dynamics of substrate translocation, and researchers have shown keen interest in elucidating the precise structural elements required for efficient OATP3 inhibition.

This class of inhibitors is of paramount importance in pharmacological research, as it sheds light on the intricate processes of cellular transport and has the potential to influence the pharmacokinetics and distribution of various substances within the body. Researchers are actively engaged in the exploration of OATP3 inhibitors to better understand their molecular interactions and structural features, thereby unraveling their potential for influencing drug disposition and physiological processes related to anionic substrates.

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)

Rifampin inhibits OATP3 by competitively binding to the transporter's substrate-binding site, thereby blocking the uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between rifampin and endogenous substrates recognized by OATP3, leading to reduced transport activity.

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 OATP3 by interacting with the transporter and disrupting its conformational changes necessary for substrate binding and transport. This interference prevents the recognition and uptake of substrates by OATP3, effectively inhibiting its transport activity.

Furosemide

54-31-9sc-203961
50 mg
$40.00
(1)

Furosemide inhibits OATP3 by binding to the transporter and disrupting its conformational changes required for substrate binding and transport. This interference prevents the recognition and uptake of substrates by OATP3, resulting in reduced transport activity.

Bosentan

147536-97-8sc-210957
10 mg
$191.00
3
(1)

Bosentan inhibits OATP3 by competitively binding to the transporter's substrate-binding site, thereby blocking the uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between bosentan and endogenous substrates recognized by OATP3, leading to reduced transport activity.

12β-Hydroxydigitoxin

20830-75-5sc-213604
sc-213604A
1 g
5 g
$140.00
$680.00
(0)

12β-Hydroxydigitoxin inhibits OATP3 by binding to the transporter and blocking its substrate-binding site, thereby preventing the recognition and uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between digoxin and endogenous substrates recognized by OATP3, leading to reduced transport activity.

Gemfibrozil

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

Gemfibrozil inhibits OATP3 by competitively binding to the transporter's substrate-binding site, thereby blocking the uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between gemfibrozil and endogenous substrates recognized by OATP3, leading to reduced transport activity.

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 inhibits OATP3 by binding to the transporter and blocking its substrate-binding site, thereby preventing the recognition and uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between erythromycin and endogenous substrates recognized by OATP3, leading to reduced transport activity.

Naringenin

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

Naringin inhibits OATP3 by competitively binding to the transporter's substrate-binding site, thereby blocking the uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between naringin and endogenous substrates recognized by OATP3, leading to reduced transport activity.

Telmisartan

144701-48-4sc-204907
sc-204907A
50 mg
100 mg
$71.00
$92.00
8
(1)

Telmisartan inhibits OATP3 by competitively binding to the transporter's substrate-binding site, thereby blocking the uptake of substrates by OATP3. This inhibition occurs due to the structural similarity between telmisartan and endogenous substrates recognized by OATP3, leading to reduced transport activity.