uptake

BMS309403 is a potent and selective inhibitor of adipocyte fatty acid binding protein aFABP. It improves endothelial function in apolipoprotein E-deficient mice and cultured human endothelial cells. It interacts with the fatty acid binding pocket inside the protein and competitively inhibits the binding of endogenous fatty acids.

Guvacine ethyl ester (Arecoline) is an alkaloid found in betel nut that is used in the synthesis of GABA uptake inhibitors.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

5-HT NA Reuptake Inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 values of 660 nM and 70 nM, respectively. It demonstrates good in vitro human metabolic stability, hERG selectivity, and passive membrane permeability [1].

Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3 Girdin Akt signaling in HCC cells.

JPH203 (KYT-0353) is a potent and specific inhibitor of L-type amino acid transporter protein 1 (LAT-1). JPH203 inhibits cellular uptake of leucine, inhibits cell proliferation, induces apoptosis, and possesses anti-inflammatory and anti-tumor activities.

N1-Acetylspermine trihydrochloride is a monoacetylated derivative of spermine which is an endogenous polyamine. N1-Acetylspermine trihydrochloride can be used in studies about the uptake of the anticancer polyamine analog bleomycin-A5 by the human carnitine transporter SLC22A16.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

SIRT6-IN-5(SIRT6 inhibitor 5) is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

Cianopramine (Ro 112465) is a selective 5-hydroxytryptamine uptake inhibitor and a tricyclic antidepressant used in the study of neurological disorders.

TMP-153 is a novel and potent ACAT inhibitor with an IC50 value of 5-10 nM for intestinal and hepatic ACAT in animals.TMP-153 has a hypocholesterolemic effect, inhibiting cholesterol uptake and lowering plasma cholesterol in rats and hamsters.

Rhizoferrin TFA is a protein secreted by Legionella pneumophila that is an iron carrier and can induce cytokine production, promote Fe(3+) uptake by wild-type Legionella pneumophila, and promote the growth of iron-deficient bacteria.

Fezolamine is a novel orally available non-tricyclic compound with antidepressant activity. It is three to two times more selective in blocking synaptosomal uptake of [3H]norepinephrine than uptake of [4H]3-hydroxytryptamine or [3H]dopamine in vitro. It blocked the inhibitory effects of rifampicin and tetraphenyl in classical behavioral tests using monoamine-depleted animals.

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

AHN 1-055 hydrochloride (3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride) is an inhibitor of dopamine transporter (DAT) and dopamine uptake(IC50 = 71 nM).

Roxindole (EMD 49980) is a selective dopamine autoreceptor and 5-HT1A dual agonist and inhibitor of 5-hydroxytryptamine (5-HT) uptake with antipsychotic and antidepressant activity.Roxindole can be used to study Parkinson's and neurodivergence.

Venuloside A (ESK246), a monoprostane glycoside from Pittosporum venulosum, is a LAT3 inhibitor and a leucine uptake inhibitor that inhibits the transporter of leucine through LAT3, and may be used in the study of prostate cancer.

Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.

Tetrofosmin is a phosphine developed to overcome the non-target uptake of radioligands by the generation of hetero-atomic compounds.

GSK2324 is a potent FXR agonist for the treatment of NAFLD by controlling hepatic lipids through reduced uptake and selective reduction of fatty acid synthesis.

ES9-17, an analog of ES9 (endosidin9), is an inhibitor of clathrin-mediated endocytosis (CME). ES9-17 inhibits the uptake of FM4-64 and transferrin. ES9-17 inhibits root growth of Arabidopsis seedings.

Copper histidine inhibited Ctr1-mediated cellular uptake of oxaliplatin in vitro without altering oxaliplatin accumulation of platinum or neurotoxicity in DRG tissues in vivo. Copper histidine is administered orally for the treatment of Menkes disease.

Suksdorfin has hypoglycemic effects, promotes adipocyte differentiation and enhances lipocalin production, activates peroxisome proliferator-activated receptor gamma (PPARγ), promotes insulin-dependent glucose uptake by adipocytes, and can be used to study obesity.