Date published: 2026-4-1

1-800-457-3801

SCBT Portrait Logo
Seach Input

OCT1 Inhibitors

Organic cation transporter 1 (OCT1) plays a pivotal role in the cellular uptake and distribution of a wide range of endogenous compounds, such as neurotransmitters, and exogenous substances, including drugs and toxins. Located primarily in the liver, kidney, and intestine, OCT1 functions as a key regulator of the intracellular concentration of cationic molecules, thereby influencing their systemic availability, metabolism, and excretion. This transporter operates through a facilitated diffusion mechanism, relying on the electrochemical gradient across the cell membrane without the direct expenditure of ATP. OCT1's activity is crucial for maintaining the homeostasis of organic cations in the body and modulating the pharmacokinetics of various drugs, highlighting its significance in both physiology and pharmacology. The inhibition of OCT1 can profoundly impact the cellular uptake and systemic disposition of its substrates, leading to alterations in their efficacy and toxicity profiles. Inhibition may occur through various mechanisms, including competitive binding, where inhibitors bind to the transporter's substrate recognition sites, curbing the access of endogenous or exogenous substrates. Additionally, non-competitive mechanisms, such as allosteric modulation, can change the transporter's conformation, reducing its activity without directly blocking the substrate binding site. Regulatory pathways involving phosphorylation or ubiquitination may also modulate OCT1 expression levels and cellular localization, indirectly influencing its transport activity.

Items 1 to 10 of 12 total

Display:

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 inhibits OCT1 indirectly by activating the pregnane X receptor (PXR), which leads to the induction of CYP3A4. The increased CYP3A4 activity metabolizes endogenous substances that would otherwise inhibit OCT1, indirectly alleviating its inhibition. T

Verapamil

52-53-9sc-507373
1 g
$374.00
(0)

Verapamil inhibits OCT1 directly by competing for binding sites, thereby reducing its substrate binding and uptake. This direct inhibition showcases the competitive nature of substrate binding to OCT1, offering insights into the structural aspects of interactions with small molecules.

Quinine

130-95-0sc-212616
sc-212616A
sc-212616B
sc-212616C
sc-212616D
1 g
5 g
10 g
25 g
50 g
$79.00
$104.00
$166.00
$354.00
$572.00
1
(0)

Quinine inhibits OCT1 directly by competing for binding sites, impeding the substrate binding and uptake. This direct inhibition underscores the competitive dynamics of substrate binding to OCT1, providing insights into the structural aspects of interactions with small molecules.

Imatinib

152459-95-5sc-267106
sc-267106A
sc-267106B
10 mg
100 mg
1 g
$26.00
$119.00
$213.00
27
(1)

Imatinib inhibits OCT1 directly by interacting with its substrate-binding sites, leading to reduced substrate uptake. This direct inhibition highlights the specific molecular interactions that can modulate OCT1 activity, offering insights into the potential of targeted therapeutics in influencing its function.

1-Adamantylamine

768-94-5sc-251475
sc-251475A
1 g
25 g
$39.00
$147.00
(0)

Amantadine inhibits OCT1 directly by interfering with substrate binding, resulting in reduced uptake. This direct inhibition exemplifies the impact of small molecules on the substrate-binding pockets of OCT1, offering insights into the structural determinants of inhibition.

Cimetidine

51481-61-9sc-202996
sc-202996A
5 g
10 g
$62.00
$86.00
1
(1)

Cimetidine inhibits OCT1 directly by competing for substrate binding, leading to decreased substrate uptake. This direct inhibition sheds light on the competitive dynamics of substrate interactions with OCT1, providing insights into the structural aspects of inhibition.

Mepyramine maleate

59-33-6sc-203629
sc-203629A
100 mg
1 g
$66.00
$224.00
1
(1)

Mepyramine maleate inhibits OCT1 directly by interfering with substrate binding, resulting in reduced substrate uptake. This direct inhibition exemplifies the impact of small molecules on the substrate-binding pockets of OCT1, offering insights into the structural determinants of inhibition.

Trimethoprim

738-70-5sc-203302
sc-203302A
sc-203302B
sc-203302C
sc-203302D
5 g
25 g
250 g
1 kg
5 kg
$67.00
$161.00
$255.00
$721.00
$3401.00
4
(1)

Trimethoprim inhibits OCT1 directly by competing for substrate binding, leading to reduced substrate uptake. This direct inhibition highlights the competitive dynamics of substrate interactions with OCT1, providing insights into the structural aspects of inhibition.

Chlorpromazine

50-53-3sc-357313
sc-357313A
5 g
25 g
$61.00
$110.00
21
(1)

Chlorpromazine inhibits OCT1 directly by interfering with substrate binding, resulting in reduced substrate uptake. This direct inhibition exemplifies the impact of small molecules on the substrate-binding pockets of OCT1, offering insights into the structural determinants of inhibition.

Propranolol

525-66-6sc-507425
100 mg
$180.00
(0)

Propranolol inhibits OCT1 directly by competing for substrate binding, leading to reduced substrate uptake. This direct inhibition showcases the competitive dynamics of substrate interactions with OCT1, providing insights into the structural aspects of inhibition.