TNF-α Antagonist III, R-7050A cell-permeable triazoloquinoxaline compound that is a TNF-α receptor antagonist

TNF-α Antagonist III, R-7050 (CAS 303997-35-5)

TNF-α Antagonist III, R-7050 | CAS 303997-35-5 is rated 5.0 out of 5 by 1.
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Synonym: 8-chloro-4-(phenylsulfanyl)-1-(trifluoromethyl)[1,2,4]triazo lo[4,3-a]quinoxaline
Application: A cell-permeable triazoloquinoxaline compound that is a TNF-α receptor antagonist
CAS Number: 303997-35-5
Purity: ≥90%
Molecular Weight: 380.77
Molecular Formula: C16H8ClF3N4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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TNF-α Antagonist III, R-7050 is a cell-permeable triazoloquinoxaline compound that is reported to act as a TNF-α receptor antagonist via the blockage of receptor-adaptor molecules complex formation and subsequent receptor internalization, but not TNF-α ligand-receptor binding. Additionally it has been shown to selectively inhibit TNF-α-, but not Fas- or C6-ceramide-, induced caspase activation and cell death in ME180 cells and exhibit higher potency against TNF-α-induced than IL-1β-induced NF-κB activation (EC50 = 0.631 and 1.45 µM, respectively) in A549 cells.


References

1. Gururaja, T.L., et al. 2007. Chem. Biol. 14: 1105-1118. PMID: 17961823

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml).
Storage :
Store at 4° C
Density :
1.59 g/cm3 (Predicted)
Refractive Index :
n20D ~1.69 (Predicted)
IC50 :
TNF-α-induced NF-κB activation: EC5050 = 0.63 µM (A549 cells); IL-1β-induced NF-κB activation : EC5050 = 1.45 µM (A549 cells)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
1486608
SMILES :
C1=CC=C(C=C1)SC2=NC3=C(C=C(C=C3)Cl)N4C2=NN=C4C(F)(F)F

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Certificate of Analysis

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TNF-α Antagonist III, R-7050  Product Citations

See how others have used TNF-α Antagonist III, R-7050. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 30150933  Fang, M.|Zhong, WH.|Song, WL.|Deng, YY.|Yang, DM.|Xiong, B.|Zeng, HK.|Wang, HD.| et al. 2018. Front Pharmacol. 9: 823.

PMID: # 28983699  Dohke, T.|Iba, K.|Hanaka, M.|Kanaya, K.|Okazaki, S.|Yamashita, T.| et al. 2018. J. Bone Miner. Metab. 36: 499-507.

PMID: # 28031332  Alqinyah, M. et al. 2017. Mol. Pharmacol. 91: 197-207.

PMID: # 27401365  Samaan, MC.|Missiuna, P.|Peterson, D.|Thabane, L.| et al. 2016. BMJ Open. 6: e011812.

PMID: # 26185049  Kirsch, AH. et al. 2015. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association. 30: 1995-2005.

PMID: # 24916922  Huang, LQ. et al. 2014. Journal of neuroinflammation. 11: 102.

Citations 1 to 6 of 6 total

How should this be stored?

Asked by: SCM4
It is important to store this product in a moisture free environment, an oxygen free environment, and under dark conditions.
Answered by: Tech Service 11
Date published: 2017-03-17
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Rated 5 out of 5 by from King King, MD. et al. (PubMed 23499961) reported that the TNF- receptor antagonist, R-7050, improves neurological outcomes following intracerebral hemorrhage in mice. -SCBT Publication Review
Date published: 2015-01-10
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