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RA 839

Names

[ CAS No. ]:
1832713-02-6

[ Name ]:
RA 839

[Synonym ]:
MFCD30182350
(3s)-1-(4-{[(2,3,5,6-Tetramethylphenyl)sulfonyl]amino}naphthalen-1-Yl)pyrrolidine-3-Carboxylic Acid
3-Pyrrolidinecarboxylic acid, 1-[4-[[(2,3,5,6-tetramethylphenyl)sulfonyl]amino]-1-naphthalenyl]-, (3S)-
(3S)-1-(4-{[(2,3,5,6-Tetramethylphenyl)sulfonyl]amino}-1-naphthyl)-3-pyrrolidinecarboxylic acid

Biological Activity

[Description]:

A noncovalent small molecule binder to Keap1 (Kd=6 uM) and selective activator of Nrf2 signaling; binds noncovalently to the Nrf2-interacting kelch domain of Keap1, significantly regulates 105 probe sets in bone marrow-derived macrophages at 10 uM; prevents the induction of both iNOS expression and nitric oxide release in response to lipopolysaccharides in macrophages; acutely induces Nrf2 target gene expression in liver in mice.

[References]

References 1. Winkel AF, et al. J Biol Chem. 2015 Nov 20;290(47):28446-55. 2. Nasiri HR, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):526-529. View Related Products by Target Keap1-Nrf2

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
707.9±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H28N2O4S

[ Molecular Weight ]:
452.566

[ Flash Point ]:
381.9±35.7 °C

[ Exact Mass ]:
452.176971

[ LogP ]:
4.94

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.656

Related Compounds