Date published: 2026-2-14

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NTCP Activators

The chemical class known as NTCP activators comprises a diverse array of compounds that modulate the activity of the sodium taurocholate cotransporting polypeptide (NTCP), a critical hepatic transporter involved in bile acid homeostasis. These activators can be categorized into direct and indirect regulators, each offering unique insights into the intricate regulatory mechanisms governing NTCP function. Direct activators, such as Dehydrocholic Acid and Lithocholic Acid, interact directly with NTCP, serving as substrates that enhance bile acid uptake. These compounds provide researchers with valuable tools to study the specific molecular interactions between NTCP and bile acids, unraveling the fine-tuned mechanisms governing hepatic bile acid transport. Indirect activators, including Rifampicin, Rosuvastatin, and GW4064, exert their influence on NTCP through various pathways. Rifampicin enhances NTCP expression by activating the pregnane X receptor (PXR), providing insights into nuclear receptor-mediated regulation of NTCP. Rosuvastatin and Ezetimibe impact NTCP through cholesterol metabolism, highlighting the interplay between lipid dynamics and NTCP regulation. GW4064, as an FXR agonist, directly activates NTCP by inducing bile acid uptake genes, showcasing the role of nuclear receptors in NTCP modulation.

Compounds like Cyclosporin A, Octreotide, and Bosentan indirectly activate NTCP through bile acid homeostasis, revealing connections between hormonal signaling and hepatic transporter regulation. Cilostazol influences NTCP via cAMP modulation, shedding light on cyclic nucleotide signaling in NTCP regulation. Carbamazepine, a drug affecting bile flow, triggers compensatory upregulation of NTCP, emphasizing the complex interplay between drug-induced changes in bile dynamics and transporter regulation. Simvastatin, an HMG-CoA reductase inhibitor, impacts NTCP through LDL receptor-mediated pathways, showcasing the integration of lipid metabolism and NTCP regulation.

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, an antibiotic, induces NTCP activity by enhancing its expression. It acts as an indirect activator by influencing nuclear receptors, especially the pregnane X receptor (PXR). Rifampicin activates PXR, leading to increased transcription of NTCP, facilitating bile acid uptake. This antibiotic provides insights into the regulatory mechanisms governing NTCP expression and its impact on bile acid homeostasis.

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)

Cyclosporin A, an immunosuppressant, indirectly activates NTCP by affecting bile acid homeostasis. It inhibits the bile salt export pump (BSEP), leading to intracellular bile acid accumulation. This triggers compensatory upregulation of NTCP, enhancing bile acid uptake. Cyclosporin A's impact on bile acid dynamics offers insights into the complex interplay between immune modulation and hepatic transporter regulation.

Octreotide Acetate

79517-01-4sc-397566
sc-397566A
sc-397566B
10 mg
25 mg
50 mg
$374.00
$454.00
$571.00
(0)

Octreotide, a somatostatin analog, indirectly activates NTCP through bile acid homeostasis. By inhibiting cholecystokinin secretion, it reduces bile release, leading to intracellular bile acid accumulation. This triggers compensatory upregulation of NTCP, facilitating bile acid uptake. Octreotide's influence on bile dynamics provides insights into the regulatory mechanisms governing NTCP and its connection to hormonal signaling.

GW 4064

278779-30-9sc-218577
5 mg
$95.00
13
(1)

GW4064 is an FXR agonist that directly activates NTCP through bile acid homeostasis. As an FXR activator, it induces the expression of genes involved in bile acid uptake, including NTCP. GW4064's direct modulation of FXR provides a tool for researchers to dissect the specific pathways governing NTCP activity and its implications for bile acid homeostasis.

Cilostazol

73963-72-1sc-201182
sc-201182A
10 mg
50 mg
$109.00
$322.00
3
(1)

Cilostazol indirectly activates NTCP by influencing intracellular cAMP levels. As a phosphodiesterase 3 inhibitor, it increases cAMP, triggering compensatory upregulation of NTCP. This modulation of cAMP dynamics impacts NTCP activity, revealing potential connections between cyclic nucleotide signaling and hepatic transporter regulation. Cilostazol's influence on intracellular signaling pathways sheds light on NTCP regulation.

Carbamazepine

298-46-4sc-202518
sc-202518A
1 g
5 g
$33.00
$71.00
5
(0)

Carbamazepine indirectly activates NTCP by modulating bile acid homeostasis. It reduces bile flow, leading to intracellular bile acid accumulation. This triggers compensatory upregulation of NTCP, facilitating bile acid uptake. Carbamazepine's impact on bile dynamics provides insights into the intricate regulatory mechanisms governing NTCP and its potential interactions with drugs affecting hepatic transporter activity.

Simvastatin

79902-63-9sc-200829
sc-200829A
sc-200829B
sc-200829C
50 mg
250 mg
1 g
5 g
$31.00
$89.00
$135.00
$443.00
13
(1)

Simvastatin indirectly activates NTCP by modulating cholesterol metabolism. As an HMG-CoA reductase inhibitor, it reduces cholesterol synthesis, triggering compensatory upregulation of LDL receptors. This, in turn, influences NTCP, as it shares regulatory pathways with LDL receptors. Simvastatin's impact on cholesterol homeostasis unveils potential connections between lipid metabolism and NTCP regulation.

Dehydrocholic acid

81-23-2sc-214863
sc-214863A
25 g
50 g
$79.00
$146.00
(1)

Dehydrocholic acid directly activates NTCP through bile acid homeostasis. As a bile acid derivative, it serves as a substrate for NTCP, enhancing bile acid uptake. Dehydrocholic acid's direct interaction with NTCP provides a tool for researchers to study the specific mechanisms governing hepatic bile acid transport and the implications for overall bile acid homeostasis.

Lithocholic acid

434-13-9sc-215262
sc-215262A
10 g
25 g
$100.00
$272.00
1
(1)

Lithocholic acid directly activates NTCP through bile acid homeostasis. As a bile acid derivative, it serves as a substrate for NTCP, enhancing bile acid uptake. Lithocholic acid's direct interaction with NTCP provides a tool for researchers to study the specific mechanisms governing hepatic bile acid transport and the implications for overall bile acid homeostasis.