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

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

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

CAS-Nr51987-99-6

Englisch Name:N-(1,3,4-Thiadiazolyl)nicotinamide

CBNumberCB92511583

SummenformelC8H6N4OS

Molgewicht206.22

MOL-Datei51987-99-6.mol

N-(1,3,4-Thiadiazolyl)nicotinamide physikalisch-chemischer Eigenschaften

Schmelzpunkt	291-293°C
Dichte	1.500±0.06 g/cm3(Predicted)
storage temp.	room temp
Löslichkeit	DMSO: ≥8mg/mL
pka	6.78±0.50(Predicted)
Aggregatzustand	powder
Farbe	white to tan
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3

Gefahreninformationscode (GHS)

N-(1,3,4-Thiadiazolyl)nicotinamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Chemische Eigenschaften
Off-White Solid
Verwenden
A thiadiazole derivative as antitumor agent.
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.
Lager
Store at RT
Einzelnachweise
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

N-(1,3,4-Thiadiazolyl)nicotinamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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