N-(1,3,4-Thiadiazolyl)nicotinamide

Description

TGN-020 (51987-99-6) is an aquaporin 4 channel blocker, IC50?= 3.1 μM.1?Reduces ischemic cerebral edema in a mouse model of focal cerebral ischemia using MRI.2?TGN-020 increases regional cerebral blood flow as determined in wild-type and AQP-4 knockout mice.3? Reduces brain edema when administered after onset of ischemia in rat models.4

Chemical properties

Off-White Solid

The Uses of N-(1,3,4-Thiadiazolyl)nicotinamide

A thiadiazole

The Uses of N-(1,3,4-Thiadiazolyl)nicotinamide

A thiadiazole derivative as antitumor agent.

What are the applications of Application

N-(1,3,4-Thiadiazolyl)nicotinamide is a thiadiazole derivative studied for its potential antitumor properties

Biochem/physiol Actions

TGN-020 is an inhibitor of Aquaporin 4 (AQP4), the most abundant water channel in brain. Aquaporins (AQPs) are water channels required for maintaining fluid homeostasis and enabling water movement across barrier membranes, but can enhance pathological cellular volume changes and cause edema in injury states. Pretreatment with the AQP4 inhibitor TGN-020 significantly reduced the volume of brain edema associated with ischemic injury in a mouse model of focal cerebral ischemia.

Storage

Store at RT

References

1) Huber?et al. (2009), Identification of aquaporin 4 inhibitors using in vitro and in silico methods; Bioorg. Med. Chem.,?17?411 2) Igarashi?et al. (2011),?Pretreatment with a novel aquaporin 4 inhibitor, TGN-020, significantly reduces ischemic cerebral edema; Neurol. Sci.,?32?113 3) Igarashi?et al. (2013),?Inhibition of aquaporin-4 significantly increases regional cerebral blood flow; Infect. Neuroreport,?24?324 4) Pirici?et al.?(2017),?Inhibition of Aquaporin-4 Improves the Outcome of Ischaemic Stroke and Modulates Brain Paravascular Drainage Pathways; Int. J. Mol. Sci.,?19?E46