OATP-H Activators
OATP-H activators are specialized chemical agents designed to enhance the activity of the Organic Anion Transporting Polypeptide H (OATP-H), a protein that functions as a transporter and is involved in the cellular uptake of a variety of organic anions, including numerous physiological substrates, drugs, and toxins. The OATP family facilitates the movement of these compounds across cell membranes, playing an essential role in their distribution and elimination in the body.
Direct activators of OATP-H typically work by binding to the transporter and inducing a conformational change that increases its affinity for substrates or its translocation rate. This could involve stabilizing the protein in an active form or altering the dynamics of the substrate binding site to increase the efficiency of substrate recognition and transport. Such activators might mimic naturally occurring ligands or interact with regions of the transporter that are critical for its activation, potentially leading to an upregulation of transport capacity. Indirect activators, in contrast, may not interact with the OATP-H protein itself but can enhance its activity by modulating the expression levels or the cellular localization of the transporter. These can include small molecules that influence the transcriptional machinery responsible for OATP-H gene expression, leading to an increase in the number of transporters synthesized by the cell. Other indirect activators may affect the transporter's post-translational modifications, such as phosphorylation or glycosylation, which can have significant impacts on its membrane trafficking, stability, and function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Indomethacin | 53-86-1 | sc-200503 sc-200503A | 1 g 5 g | $29.00 $38.00 | 18 | |
Indomethacin is an inhibitor of prostaglandin-endoperoxide synthase (COX). The inhibition of COX reduces the synthesis of prostaglandin E2 (PGE2), a molecule known to downregulate OATP-H function. With less PGE2, OATP-H can perform more transport cycles, enhancing its activity. | ||||||
Zileuton | 111406-87-2 | sc-204417 sc-204417A sc-204417B sc-204417C | 10 mg 50 mg 1 g 75 g | $84.00 $307.00 $369.00 $1254.00 | 8 | |
Zileuton is an inhibitor of 5-lipoxygenase, reducing the production of leukotrienes, inflammatory molecules that can decrease OATP-H function. By reducing leukotriene levels, Zileuton can indirectly enhance the functional activity of OATP-H. | ||||||
Probenecid | 57-66-9 | sc-202773 sc-202773A sc-202773B sc-202773C | 1 g 5 g 25 g 100 g | $28.00 $39.00 $100.00 $277.00 | 28 | |
Probenecid is a competitive inhibitor of organic anion transporters but has been shown to increase the expression of OATP-H. It is hypothesized that this could be due to cellular compensation mechanisms, leading to an indirect increase in OATP-H activity. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $374.00 | ||
Verapamil is a calcium channel blocker. By modulating calcium levels, it can influence the function of OATP-H, as calcium is known to play a role in the regulation of organic anion transporters. | ||||||
Chlorpromazine | 50-53-3 | sc-357313 sc-357313A | 5 g 25 g | $61.00 $110.00 | 21 | |
Chlorpromazine is a dopamine antagonist. It is hypothesized that it could increase the functional activity of OATP-H as dopamine has been linked to the regulation of organic anion transporters. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $110.00 $250.00 $936.00 $50.00 | 33 | |
Quercetin is a plant flavonoid known to inhibit the function of several organic anion transporters. However, it has been shown to increase the activity of OATP-H, possibly due to cellular compensation mechanisms. | ||||||
Losartan | 114798-26-4 | sc-353662 | 100 mg | $130.00 | 18 | |
Losartan is an angiotensin II receptor antagonist. Angiotensin II has been shown to downregulate the function of several organic anion transporters. By antagonizing angiotensin II, Losartan can indirectly enhance the functional activity of OATP-H. | ||||||
Rosuvastatin | 287714-41-4 | sc-481834 | 10 mg | $145.00 | 8 | |
Rosuvastatin is a statin drug that has been shown to increase the functional activity of OATP-H. The exact mechanism is not known but it is believed to involve changes in cellular lipid composition that favor OATP-H function. | ||||||
Olmesartan Medoxomil | 144689-63-4 | sc-219482 sc-219482A | 10 mg 100 mg | $60.00 $186.00 | ||
Olmesartan is an angiotensin II receptor antagonist. By antagonizing the effects of angiotensin II, which has been shown to downregulate the function of several organic anion transporters, Olmesartan can indirectly enhance the functional activity of OATP-H. | ||||||
Omeprazole | 73590-58-6 | sc-202265 | 50 mg | $67.00 | 4 | |
Omeprazole is a proton pump inhibitor that increases gastric pH. This could enhance the activity of OATP-H, as it has been suggested that changes in intracellular pH can modulate the function of organic anion transporters. | ||||||