R-7050 Struktur

R-7050

Bezeichnung:R-7050

CAS-Nr303997-35-5

Englisch Name:R-7050

CBNumberCB53152725

SummenformelC16H8ClF3N4S

Molgewicht380.77

MOL-Datei303997-35-5.mol

R-7050 physikalisch-chemischer Eigenschaften

Dichte	1.59±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	insoluble in H2O; ≥17.67 mg/mL in DMSO; ≥2.2 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	crystalline solid
pka	-3.70±0.30(Predicted)
Farbe	Light yellow to yellow

R-7050 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
R 7050 is a cell permeable TNF-α receptor antagonist.
Biologische Aktivität
ec50: 0.631 μm by tnf-α by icam-1 elisa assayr-7050 is a tnf-α receptor signaling antagonist.tnf-α induces biological activity throgh stimulation of the tumor necrosis factor receptor. although plenty of pre-clinical and clinical evidence suggests a detrimental role, small molecule tnf-αsignaling pathway inhibitors remain largely unexplored in the context of a brain hemorrhage.
in vitro
r-7050 was identified as a selective inhibitot of tnf-α induced cellular signaling by using differential library screening. unlike biologic tnf inhibitors directly binding tnf-α, r-7050 could not affect binding of tnf-α to tnfr. in contrast, r-7050 was able to selectively inhibit the association of tnf receptor with intracellular adaptor molecules [1].
in vivo
in previous animal study, r-7050 was tested to attenuate neurovascular injury after intracerebral hemorrhage (ich) in mice. results showed that up to 2h post-injury administration of r-7050 was able to significantly reduce blood-brain barrier opening and attenuate edema development at 24h post-ich. in addition, neurological outcomes were also improved over the first 3 days after injury. whereas, r-7050 was not found to be albe to reduce hematoma volume, indicating the beneficial effects of tnfr inhibition were downstream of clot formation/resolution [2].
Lager
Store at +4°C
Einzelnachweise
[1] gururaja tl, yung s, ding r, huang j, zhou x, mclaughlin j, daniel-issakani s, singh r, cooper rd, payan dg, masuda es, kinoshita t. a class of small molecules that inhibit tnfalpha-induced survival and death pathways via prevention of interactions between tnfalphari, tradd, and rip1. chem biol. 2007 oct;14(10):1105-18.
[2] king md, alleyne ch jr, dhandapani km. tnf-alpha receptor antagonist, r-7050, improves neurological outcomes following intracerebral hemorrhage in mice. neurosci lett. 2013 may 10;542:92-6.

R-7050 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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