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).

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.

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

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.

Oxfendazole (RS-8858), a broad spectrum benzimidazole anthelmintic, protects livestock against roundworm, strongyles and pinworms.

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a potent inhibitor of dopamine uptake (IC50: 1-51 nM).

BAMB-4 (ITPKA-IN-C14) is a highly membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA), effectively suppressing the metastasis-promoting effect of ITPKA in lung tumor cells (with IC50 of 37 μM in ADP-Glo Assay).

NO-711ME (N-O711 Methyl ester) is a prodrug of NO-711. It also is a potent and selective GABA uptake inhibitor.

Hydroxybupropion is the major active metabolite of Bupropion and an antagonist of nACh receptor. Hydroxybupropion inhibits norepinephrine uptake (IC50 = 1.7 μM).

NBTGR is a potent nucleoside transport inhibitor(adenosine uptake ,Ki of 70 nM).

Riluzole hydrochloride (PK 26124 hydrochloride) is an anticonvulsant compound belonging to the family of sodium channel blockers that inhibits GABA uptake.Riluzole hydrochloride is a sodium-glutamate antagonist with anticancer and neuroprotective activity and can be used to study amyotrophic lateral sclerosis and neurological disorders.

Tiagabine hydrochloride (NO050328 hydrochloride) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.