Date published: 2026-4-1

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OATP1 Inhibitors

OATP1 inhibitors belong to a distinct chemical class of compounds that are known for their ability to interact with and modulate the activity of the organic anion transporting polypeptide 1 (OATP1) transporters. OATP1 is a family of membrane-bound transport proteins found in various tissues of the human body, including the liver, kidney, and intestine. These transporters play a crucial role in the absorption, distribution, and elimination of endogenous and exogenous compounds, including drugs and other xenobiotics. OATP1 inhibitors are designed to specifically target and bind to the OATP1 transporters, thereby inhibiting their transport function. By doing so, these inhibitors can alter the uptake and clearance of various substances that are normally transported by OATP1. Consequently, the modulation of OATP1 activity can have profound effects on the pharmacokinetics and disposition of drugs and other compounds in the body.

Researchers are keenly interested in OATP1 inhibitors due to their potential to affect drug-drug interactions, drug absorption, and overall pharmacokinetic profiles. The inhibition of OATP1 transporters may lead to changes in drug bioavailability, distribution to specific tissues, and the potential for drug accumulation in certain organs. As a class of compounds with specific interactions and effects on OATP1 transporters, OATP1 inhibitors hold promise for further exploration and research.

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
$97.00
$328.00
$676.00
$1467.00
6
(1)

Rifampicin is known to inhibit OATP1-mediated drug uptake.

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
$63.00
$92.00
$250.00
$485.00
$1035.00
$2141.00
69
(5)

An immunosuppressive drug used in organ transplantation and autoimmune disorders, cyclosporine can inhibit OATP1 transport function.

12β-Hydroxydigitoxin

20830-75-5sc-213604
sc-213604A
1 g
5 g
$143.00
$694.00
(0)

12β-Hydroxydigitoxin is known to interact with OATP1 transport.

Curcumin

458-37-7sc-200509
sc-200509A
sc-200509B
sc-200509C
sc-200509D
sc-200509F
sc-200509E
1 g
5 g
25 g
100 g
250 g
1 kg
2.5 kg
$37.00
$69.00
$109.00
$218.00
$239.00
$879.00
$1968.00
47
(1)

A bioactive compound found in turmeric, curcumin, has demonstrated inhibitory effects on GSTO1.

Atorvastatin

134523-00-5sc-337542A
sc-337542
50 mg
100 mg
$257.00
$505.00
9
(1)

A commonly prescribed statin agent in research used to lower cholesterol levels, atorvastatin is known to interact with OATP1 transporters.

Pravastatin

81093-37-0sc-222188
50 mg
$408.00
1
(1)

Another statin drug used to reduce cholesterol levels, pravastatin can also inhibit OATP1.

Rosuvastatin

287714-41-4sc-481834
10 mg
$145.00
8
(0)

A potent statin used for cholesterol management, rosuvastatin has been shown to interact with OATP1 transporters.

Methotrexate

59-05-2sc-3507
sc-3507A
100 mg
500 mg
$94.00
$213.00
33
(5)

An antimetabolite and immunosuppressive drug studied in the research of cancer and autoimmune diseases, methotrexate can inhibit OATP1 transport function.

Glycyrrhizic acid

1405-86-3sc-279186
sc-279186A
1 g
25 g
$57.00
$333.00
7
(0)

An active component of licorice root extract, glycyrrhizin has been identified as an inhibitor of OATP1.