SKF 96365 HYDROCHLORIDE Struktur

SKF 96365 HYDROCHLORIDE

Bezeichnung:SKF 96365 HYDROCHLORIDE

CAS-Nr130495-35-1

Englisch Name:SKF 96365 HYDROCHLORIDE

CBNumberCB7752278

SummenformelC22H27ClN2O3

Molgewicht402.91

MOL-Datei130495-35-1.mol

SKF 96365 HYDROCHLORIDE physikalisch-chemischer Eigenschaften

Schmelzpunkt	119 °C
RTECS-Nr.	NI6823500
storage temp.	Inert atmosphere,Room Temperature
Löslichkeit	H₂O: >20 mg/mL
Aggregatzustand	solid
Farbe	white
Wasserlöslichkeit	Soluble to 100mM in water
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
CAS Datenbank	130495-35-1(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36
WGK Germany	3
HS Code	2933.29.4300

Gefahreninformationscode (GHS)

SKF 96365 HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
SKF-96365 (130495-35-1) is an inhibitor of receptor-mediated calcium entry (RMCE) with IC50‘s of 8.5 μM for ADP stimulated platelets and 11.7 μM for thrombin stimulated platelets. Also inhibits Voltage-gated Ca2+ but not ATP-gated Ca2+ entry.1 It has also been shown to block transient receptor potential canonical type (TRPC) channels2, high-voltage-activated (HVA) L-type channels1, K channels3, sarcoplasmic reticulum Ca-ATPase4 and voltage-gated sodium channels5. SKF-96365 is a potent blocker of LVA T-type Ca channels, in particular Ca(V)3.1 (IC50 = 0.56 μM).6
Verwenden
SKF 96365 Hydrochloride is a novel inhibitor of receptor-mediated calcium entry.
Definition
ChEBI: SKF-96365 hydrochloride is the hydrochloride salt of SKF-96365. It is a TRP channel blocker. It has a role as a TRP channel blocker, an apoptosis inducer, an autophagy inducer, a GABA antagonist, an antineoplastic agent, a calcium channel blocker and a platelet aggregation inhibitor. It contains a SKF-96365 free base(1+).
Allgemeine Beschreibung
Inhibits receptor-mediated Ca²⁺ entry in stimulated platelets (IC₅₀ = 8-12 μM in intact platelets), neutrophils, and endothelial cells (IC₅₀ = 30 μM for human endothelial cells) at concentrations that do not affect internal Ca²⁺ release. Also inhibits voltage-gated Ca²⁺ entry in excitable cells. Inhibits the histamine-induced formation of nitric oxide in human endothelial cells.
Biologische Aktivität
Store-operated Ca 2+ entry (SOCE) inhibitor that inhibits STIM1. Also inhibits TRP channels, voltage-gated Ca 2+ channels and potassium channels.
Biochem/physiol Actions
SKF-96365 with an alkylated imidazole ring is a selective inhibitor of receptor-mediated Ca2+?entry and voltage-gated Ca2+?entry . SKF-96365 mediated depolarization of smooth cardiac muscle membrane and had no impact on the acetylcholine (ACh)-induced depolarization. It is an inhibitor for SOCE (store-operated calcium entry). It also inhibits Homer1 protein expression. SKF-96365 elicits protective functionality in 1-methyl-4-phenylpyridinium(MPP) mediated cytotoxicity.
Lager
Store at RT
Einzelnachweise
1) Merritt et al.,(1990) SKF96365, a novel inhibitor of receptor-mediated calcium entry; Biochem. J. 271 515 2) Kiselyov et al., (1998) Functional interaction between InsP3 receptors and store-operated Htrp3 channels; Nature, 396 478 3) Schwarz et al., (1994) Multiple effects of SKF96365 on ionic currents and intracellular calcium in human endothelial cells; Cell Calcium, 15 45 4) Mason et al., (1993) Inhibition of Ca2+ transport pathways in thymic lymphocytes by econazole, miconazole and SKF96365; Am. J. Physiol., 264 C654 5) Hong et al. (1994) Inhibition of the sodium channel by SKF96365, an inhibitor of the receptor-operated calcium channel, in mouse diaphragm; J. Biomed. Sci., 1 172 6) Singh et al.,(2010) The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels; Br. J. Pharmacol., 160 1464

SKF 96365 HYDROCHLORIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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