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

TGN-020 (51987-99-6) is an aquaporin 4 channel blocker, IC50= 3.1 μM.1Reduces ischemic cerebral edema in a mouse model of focal cerebral ischemia using MRI.2TGN-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

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A thiadiazole derivative as antitumor agent.

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.

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[1] VINCENT J. HUBER  Tsutomu N  Mika Tsujita. Identification of Aquaporin 4 inhibitors using in vitro and in silico methods[J]. Bioorganic & Medicinal Chemistry, 2009, 17 1: Pages 411-417. DOI:10.1016/j.bmc.2007.12.040
[2] HIRONAKA IGARASHI. Pretreatment with a novel aquaporin 4 inhibitor, TGN-020, significantly reduces ischemic cerebral edema.[J]. Neurological Sciences, 2011, 32 1: 113-116. DOI:10.1007/s10072-010-0431-1
[3] HIRONAKA IGARASHI. Inhibition of aquaporin-4 significantly increases regional cerebral blood flow.[J]. Neuroreport, 2013, 24 6: 324-328. DOI:10.1097/wnr.0b013e32835fc827
[4] IONICA PIRICI. Inhibition of Aquaporin-4 Improves the Outcome of Ischaemic Stroke and Modulates Brain Paravascular Drainage Pathways.[J]. International Journal of Molecular Sciences, 2017, 19 1. DOI:10.3390/ijms19010046