Nucleoside Transporters

CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.

Soluflazine is a nucleoside transport inhibitor with anticonvulsant action. Soluflazine can be used as an antiepileptic agent.

Draflazine (R-75231) is a ENT1 inhibitor.

KF24345 free base is an orally active inhibitor of adenosine uptake. It effectively inhibits adenosine uptake in erythrocytes from humans, mice, rabbits, and hamsters, demonstrating IC50 values of 59.5, 130.1, 104.2, and 30.9 nM, respectively. Additionally, KF24345 free base exhibits anti-inflammatory properties by inhibiting lipopolysaccharide (LPS)-induced production of TNF-α and preventing leukopenia in murine models, making it a valuable tool for research in inflammatory responses and adenosine signaling pathways.

(S)-Draflazine is a selective nucleoside transport blocker that effectively inhibits nucleoside uptake. This compound demonstrates significant biological activity in modulating nucleoside transport mechanisms. (S)-Draflazine is utilized in research contexts to study nucleoside-related processes and their implications in various biological pathways and diseases.

Dilazep dihydrochloride is an adenosine uptake inhibitor that promotes vasodilation in cerebral and coronary circulation by enhancing the effects of adenosine. This compound exhibits protective properties against ischemic damage, reduces platelet aggregation, and interferes with the membrane transport of nucleosides. It is valuable in research applications focused on cardiovascular physiology and neurological protection.

hENT4-IN-1 is a selective inhibitor of the human equilibrative nucleoside transporter 4 (ENT4), exhibiting an IC50 of 74.4 nM. This compound is crucial for investigating the biological roles of ENT4 in cellular nucleoside transport and metabolism. Its application extends to studies evaluating the impact of ENT4 inhibition on various physiological and pathological processes, making it a valuable tool for research in cancer biology and therapeutic development.

FPMINT is a potent, irreversible, and non-competitive inhibitor of Equilibrative Nucleoside Transporters (ENTs), with a higher selectivity for ENT2 compared to ENT1. By effectively blocking ENT2, FPMINT significantly impacts uridine uptake, making it a valuable tool in studies related to nucleoside transport mechanisms. Its application in research can aid in elucidating the physiological roles of ENT2 in various biological processes.

Dilazep is an adenosine uptake inhibitor that enhances the effects of adenosine, leading to cerebral and coronary vasodilation. This compound not only reduces ischemic damage but also inhibits platelet aggregation and the membrane transport of nucleosides. Dilazep is useful in research applications focused on cardiovascular physiology and neuroprotection.

dMeThPmR is a selective inhibitor of the human nucleoside transporter 1 (hCNT1), exhibiting a potent inhibitory constant (Ki) in the range of 0.3-0.98 μM. While dMeThPmR shows minimal inhibition of hCNT2 (IC50 = 133 μM) and hCNT3 (Ki = 32.7 μM), it effectively protects cells from the cytotoxic effects of nucleoside drugs. This compound is valuable for research on cancer and related therapies, providing insights into nucleoside transport mechanisms and drug interactions.

MeThPmR is a potent and selective inhibitor of the human nucleoside transporter 1 (hCNT1) with a Ki ranging from 0.16 to 0.69 μM. It exhibits minimal inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR has been demonstrated to provide protection against the cytotoxic effects of nucleoside drugs, making it a valuable tool for cancer research applications.