2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Struktur

2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE

Bezeichnung:2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE

CAS-Nr182004-65-5

Englisch Name:2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE

CBNumberCB6422033

SummenformelC17H21N3O6S2

Molgewicht427.49

MOL-Datei182004-65-5.mol

2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE physikalisch-chemischer Eigenschaften

Schmelzpunkt	>214°C (dec.)
storage temp.	Inert atmosphere,2-8°C
Löslichkeit	Soluble in DMSO (up to 50 mg/ml).
Aggregatzustand	White crystalline solid
Farbe	Tan
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

HS Code

2930.90.2900

Gefahreninformationscode (GHS)

2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
KB-R7943 (182004-65-5) is a potent and selective inhibitor of the reversed Na+/Ca2+ exchanger (NCE or NCX; IC50‘s = 1.2-2.4 μM in cardiomyocytes, smooth muscle cells, NCX1-transfected fibroblasts1; 0.7 μM in cultured rat forebrain2). KB-R7943 has also been shown to inhibit the mitochondrial Ca2+ uniporter (MCU) Ki = 5.5 μM.3 Recently shown to inhibit complex I in the mitochondrial respiratory chain (IC50 = 11.4 μM) and block NMDA receptors (IC50 = 13.4 μM).4
Verwenden
KB-R7943 Mesylate is a selective inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1.
Allgemeine Beschreibung
A cell-permeable inhibitor of the influx/reverse mode of the Na⁺/Ca²⁺ exchanger (NCX) (IC₅₀ = 4.3 μM for NCX1, 4.7 μM for NCX2, and 1.4 μM for NCX3). Directly modulates Na⁺/Mg²⁺ exchange in a Ca²⁺-dependent manner. Reported ot offer neuronal and cardio-protection against ischemic injury. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC₅₀<10 μM).
Biologische Aktivität
Potent, selective inhibitor of the reverse mode of the Na + /Ca 2+ exchanger (IC 50 = 0.7 mM). Does not affect Na + -dependent transport systems, Na + channels or ionotropic glutamate receptors.
Biochem/physiol Actions
Target IC50: 4.3 μM, 4.7 μM, and 1.4 μM for NCX1,NCX2, and NCX3, respectively
Lager
Room temperature
Einzelnachweise
1) Iwamoto et al. (1996), Novel Isothiourea Derivative Selectively Inhibits the Reverse Mode of Na+/Ca2+ Exchange in Cells Expressing NCX1; J. Biol .Chem., 271 22391 2) Hoyt et al. (1998) Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons; Mol. Pharmacol., 53 742 3) Santo-Domingo et al. (2007) The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter; Br. J. Pharmacol., 151 647 4) Brustovetsky et al. (2011) KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I; Br. J. Pharmacol,. 162 255

2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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