|
|
| Product Name: | R-7050 | | Synonyms: | R-7050;R-7050;R 7050;R7050;8-Chloro-4-(phenylthio)-1-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]quinoxaline;TNF-α Antagonist III;[1,2,4]Triazolo[4,3-a]quinoxaline, 8-chloro-4-(phenylthio)-1-(trifluoromethyl)-;TNF-alpha Antagonist III, R-7050;TNF-α Antagonist III;R 7050,Inhibitor,R7050,inhibit,TNFR,Tumor Necrosis Factor Receptor,TNF Receptor,R-7050 | | CAS: | 303997-35-5 | | MF: | C16H8ClF3N4S | | MW: | 380.77 | | EINECS: | | | Product Categories: | | | Mol File: | 303997-35-5.mol |  |
| | R-7050 Chemical Properties |
| density | 1.59±0.1 g/cm3(Predicted) | | storage temp. | Sealed in dry,Store in freezer, under -20°C | | solubility | insoluble in H2O; ≥17.67 mg/mL in DMSO; ≥2.2 mg/mL in EtOH with gentle warming and ultrasonic | | form | crystalline solid | | pka | -3.70±0.30(Predicted) |
| | R-7050 Usage And Synthesis |
| Uses | R 7050 is a cell permeable TNF-α receptor antagonist. | | Biological Activity | 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]. | | storage | Store at +4°C | | references | [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 Preparation Products And Raw materials |
|