Amino acid Transporter Inhibitor

DOPE (Dioleoylphosphatidylethanolamine; 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine) is an orally active inhibitor of ferroptosis with anti-inflammatory and intestinal barrier maintenance activities. DOPE regulates the expression of ACSL4, SLC7A11 and GPX4 to restore the redox system balance, thereby reducing the levels of lipid peroxides, iron ions and intestinal inflammatory factors (IL-1β and IL-6). DOPE promotes the migration and proliferation of intestinal epithelial cells and increases the level of tight junction proteins; it also destabilizes endosomal membranes, mediates the conjugation of RVG peptides with mesenchymal stem cell-derived exosomes to enhance brain targeting. DOPE can be applied to research related to neonatal necrotizing enterocolitis and Alzheimer's disease.

KMH-233, a potent, reversible and selective inhibitor of l-type amino acid transporter LAT1/SLC7A5, inhibits the uptake of LAT1 substrate, l-leucin (IC₅₀=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).

JNT-517 is an orally active, selective SLC6A19 allosteric inhibitor with an IC₅₀ of 47 nM for human SLC6A19. JNT-517 can be used for the study of phenylketonuria (PKU).

DOPE GMP is DOPE (HY-112005) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DOPE (Dioleoylphosphatidylethanolamine; 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine) is an orally active inhibitor of ferroptosis with anti-inflammatory and intestinal barrier maintenance activities. DOPE regulates the expression of ACSL4, SLC7A11 and GPX4 to restore the redox system balance, thereby reducing the levels of lipid peroxides, iron ions and intestinal inflammatory factors (IL-1β and IL-6). DOPE promotes the migration and proliferation of intestinal epithelial cells and increases the level of tight junction proteins; it also destabilizes endosomal membranes, mediates the conjugation of RVG peptides with mesenchymal stem cell-derived exosomes to enhance brain targeting. DOPE can be applied to research related to neonatal necrotizing enterocolitis and Alzheimer's disease.

Cinromide is an anticonvulsant agent. Cinromide inhibits epithelial neutral amino acid transporter B⁰AT1 (SLC6A19) with an IC₅₀ of 0.5 μM.

LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction.

JX237 is an inhibitor of the epithelial neutral amino acid transporter B⁰AT1 (SLC6A19) with an IC₅₀ value of 31 nM. SLC6A19 is the main transporter for the absorption of neutral amino acids in the intestines and their reabsorption in the kidneys. By inhibiting B⁰AT1, JX237 can be used for the study of disorders of amino acid metabolism.

PROT-IN-1 is a PROT inhibitor (IC₅₀: 1.48 μM). PROT-IN-1 is applicable to research related to cognitive impairment.

SLC6A19-IN-4 is an allosteric-competitive and orally active B⁰AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B⁰AT1 with IC₅₀ values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B⁰AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research.

AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is an AKR1B1/STAT3/SLC7A11 regulator that reverses DOX resistance in MCF-7/ADR cells by enhancing ferroptosis activity. AKR1B1/STAT3/SLC7A11-regulator-1 can be used in breast cancer research.

SLC6A19-IN-3 (Compound 83-P1-P2) is a potent, selective and orally active SLC6A19 inhibitor with an IC₅₀ of 28 nM. SLC6A19-IN-3 can block SLC6A19-mediated transmembrane transport of phenylalanine, reducing intestinal absorption of phenylalanine from food and renal tubular reabsorption of phenylalanine. SLC6A19-IN-3 can be used for the research of metabolic disease, such as phenylketonuria.

JN-170 is a potent and highly selective inhibitor and transport corrector of human SLC6A19 (IC₅₀=47 nM). Furthermore, at a concentration of 35 μM, JN-170 exhibits no activity against SLC1A5, SLC7A5, or SLC6A8. JN-170 is applicable to research on phenylketonuria (PKU) and hyperphenylalaninemia. JN-170 is also suitable for studies related to various metabolic disorders, including tyrosinemia, maple syrup urine disease, urea cycle disorders, and hyperammonemia.

LP-403812 is a high affinity proline transporter (PROT) inhibitor that produces dose-dependent inhibition of hPROT (IC₅₀=0.11 μM; K_i=0.12 μM) and also inhibits the activity of mouse brain synaptosomal mPROT with the same potency (IC₅₀=0.23 μM). LP-403812 can be used to study the function of PROT in the brain.

Creatine transporter-IN-1 is a synthetic creatine transporter (CT1/SLC6A8) inhibitor. Creatine transporter-IN-1 inhibits creatine uptake and shows anticancer activity against cancer cells.

SLC6A19-IN-2 (Example 4) is a potent SLC6A19 inhibitor with an IC₅₀ of 14 nM. SLC6A19-IN-2 can be used for the study of metabolic diseases such as nonalcoholic steatohepatitis (NASH), nonalcoholic fatty liver disease (NAFLD) and phenylketonuria (PKU).

α,α-DiBn-DL-Gly (Dibenzylglycine) is an achiral α-substituted phenylalanine derivative, non-substrate weak inhibitor of LAT1 (L-type amino acid transporter 1). α,α-DiBn-DL-Gly does not stimulate efflux of-Gabapentin from preloaded HEK-hLAT1 cells. α,α-DiBn-DL-Gly shows minimal inhibition of-Gabapentin (HY-A0057) uptake into HEK-hLAT1 cells.

SLC6A19-IN-5 (Example 25) is a SLC6A19 inhibitor with an IC₅₀ of 11 nM. SLC6A19-IN-5 can be used for research on diseases related to abnormal amino acid metabolism, amino acid transport, and/or amino acid levels.

LX-6171 is an orally active SLC6A7 inhibitor. LX-6171 can be used to study diseases characterized by cognitive impairment, such as Alzheimer's disease, schizophrenia or vascular dementia.