uptake

V-9302 (V9302) is a competitive antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 (IC50: 9.6 uM).

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

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

Oxolinic acid (Nidantin) is a synthetic antimicrobial related to NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive, and orally active pan-PTP (protein tyrosine phosphatases) inhibitor with insulin-mimicking effects and anti-diabetic properties. BMOV is a potent insulin sensitizer and has been shown to improve cardiac dysfunctions in diabetic models. BMOV inhibits HCPTPA, PTP1B, HPTPβ, and SHP2 with IC50s of 126 nM, 109 nM, 26 nM, and 201 nM, respectively [1][2].

DMT1 blocker 2, compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 hydrogen peroxide value of 0.83, which is expected to block iron uptake by intestinal epithelial cells in vivo.

LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing [hGlyT1a].

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

SLC13A5-IN-1 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5) that completely blocks the uptake of 14C-citrate, with an IC50 of 0.022 μM in HepG2 cells.

Dilazep dihydrochloride is an adenosine uptake inhibitor. It also inhibits ischemic damage, membrane transport of nucleosides, and platelet aggregation. It has cerebral and coronary vasodilating action through the enhancement of the effect of adenosine.

LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). LY2183240 is a novel and highly effective blocker of anandamide uptake (IC50 = 270 pM).

Nisoxetine hydrochloride is a noradrenaline transporter (NET) inhibitor

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.

Arecaidine hydrochloride may have carcinogenesis.

MCU-i4 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.

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

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].

Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride), a widely used anti-diabetic drug, exhibits potential anti-Y properties by inhibiting the proliferation of various Y cells, including colon and prostate.

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.

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.

Galidesivir (BCX4430) is a broad-spectrum antiviral compound, an adenosine analog that inhibits viral RNA-dependent RNA polymerase (RdRp) activity.Galidesivir inhibits a wide range of RNA viral pathogens in vitro, and reduces lung infections in infected animals.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.