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.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $97.00 $328.00 $676.00 $1467.00 | 6 | |
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 | 59865-13-3 | sc-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 | |
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 | 79517-01-4 | sc-397566 sc-397566A sc-397566B | 10 mg 25 mg 50 mg | $374.00 $454.00 $571.00 | ||
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 | 278779-30-9 | sc-218577 | 5 mg | $95.00 | 13 | |
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 | 73963-72-1 | sc-201182 sc-201182A | 10 mg 50 mg | $109.00 $322.00 | 3 | |
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 | 298-46-4 | sc-202518 sc-202518A | 1 g 5 g | $33.00 $71.00 | 5 | |
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 | 79902-63-9 | sc-200829 sc-200829A sc-200829B sc-200829C | 50 mg 250 mg 1 g 5 g | $31.00 $89.00 $135.00 $443.00 | 13 | |
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 | 81-23-2 | sc-214863 sc-214863A | 25 g 50 g | $79.00 $146.00 | ||
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 | 434-13-9 | sc-215262 sc-215262A | 10 g 25 g | $100.00 $272.00 | 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. | ||||||