RA-839
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MedKoo CAT#: 561359

CAS#: 1832713-02-6

Description: RA-839 is a noncovalent small molecule binder to Keap1 and selective activator of Nrf2 signaling. RA-839 also suppresses LPS-induced iNOS and nitric oxide expression in macrophages.


Chemical Structure

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RA-839
CAS# 1832713-02-6

Theoretical Analysis

MedKoo Cat#: 561359
Name: RA-839
CAS#: 1832713-02-6
Chemical Formula: C25H28N2O4S
Exact Mass: 452.18
Molecular Weight: 452.570
Elemental Analysis: C, 66.35; H, 6.24; N, 6.19; O, 14.14; S, 7.08

Price and Availability

Size Price Availability Quantity
10mg USD 385 2 weeks
50mg USD 1250 2 weeks
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Synonym: RA-839; RA 839; RA839;

IUPAC/Chemical Name: (3S)-1-[4-[[(2,3,5,6-Tetramethylphenyl)sulfonyl]amino]-1-naphthalenyl]-3-pyrrolidinecarboxylic acid

InChi Key: BVYWIQHJXAEJOD-IBGZPJMESA-N

InChi Code: InChI=1S/C25H28N2O4S/c1-15-13-16(2)18(4)24(17(15)3)32(30,31)26-22-9-10-23(21-8-6-5-7-20(21)22)27-12-11-19(14-27)25(28)29/h5-10,13,19,26H,11-12,14H2,1-4H3,(H,28,29)/t19-/m0/s1

SMILES Code: O=C([C@@H]1CN(C2=C3C=CC=CC3=C(NS(=O)(C4=C(C)C(C)=CC(C)=C4C)=O)C=C2)CC1)O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: RA 839 is an Nrf2 activator; it inhibits Nrf2/Keap1 interaction (Kd = 6 μM). RA 839 suppresses LPS-induced iNOS and nitric oxide expression in macrophages and is anti-inflammatory.
In vitro activity: RA-839 inhibits Rotavirus (RV) RNA and protein expression, viroplasm formation, yield of virion progeny and virus-induced cytopathy independent of RV strains. This study demonstrates that RA-839 is a potent antagonist of RV propagation in vitro and can be developed as anti-rotaviral therapeutics. Reference: Antiviral Res. 2019 Jan;161:53-62. https://pubmed.ncbi.nlm.nih.gov/30465784/
In vivo activity: RA839 prevented the induction of both inducible nitric-oxide synthase expression and nitric oxide release in response to lipopolysaccharides in macrophages. In mice, RA839 acutely induced Nrf2 target gene expression in the liver. RA839 is a selective inhibitor of the Keap1/Nrf2 interaction and a useful tool compound to study the biology of Nrf2. Reference: J Biol Chem. 2015 Nov 20;290(47):28446-28455. https://pubmed.ncbi.nlm.nih.gov/26459563/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.3 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 452.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Patra U, Mukhopadhyay U, Sarkar R, Mukherjee A, Chawla-Sarkar M. RA-839, a selective agonist of Nrf2/ARE pathway, exerts potent anti-rotaviral efficacy in vitro. Antiviral Res. 2019 Jan;161:53-62. doi: 10.1016/j.antiviral.2018.11.009. Epub 2018 Nov 19. PMID: 30465784. 2. Winkel AF, Engel CK, Margerie D, Kannt A, Szillat H, Glombik H, Kallus C, Ruf S, Güssregen S, Riedel J, Herling AW, von Knethen A, Weigert A, Brüne B, Schmoll D. Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling. J Biol Chem. 2015 Nov 20;290(47):28446-28455. doi: 10.1074/jbc.M115.678136. Epub 2015 Oct 12. PMID: 26459563; PMCID: PMC4653701.
In vitro protocol: 1. Patra U, Mukhopadhyay U, Sarkar R, Mukherjee A, Chawla-Sarkar M. RA-839, a selective agonist of Nrf2/ARE pathway, exerts potent anti-rotaviral efficacy in vitro. Antiviral Res. 2019 Jan;161:53-62. doi: 10.1016/j.antiviral.2018.11.009. Epub 2018 Nov 19. PMID: 30465784.
In vivo protocol: 1. Winkel AF, Engel CK, Margerie D, Kannt A, Szillat H, Glombik H, Kallus C, Ruf S, Güssregen S, Riedel J, Herling AW, von Knethen A, Weigert A, Brüne B, Schmoll D. Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling. J Biol Chem. 2015 Nov 20;290(47):28446-28455. doi: 10.1074/jbc.M115.678136. Epub 2015 Oct 12. PMID: 26459563; PMCID: PMC4653701.

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1: Nasiri HR, Linge S, Ullmann D. Thermodynamic profiling of inhibitors of Nrf2:Keap1 interactions. Bioorg Med Chem Lett. 2016 Jan 15;26(2):526-529. doi: 10.1016/j.bmcl.2015.11.082. Epub 2015 Nov 23. PubMed PMID: 26653613.

2: Winkel AF, Engel CK, Margerie D, Kannt A, Szillat H, Glombik H, Kallus C, Ruf S, Güssregen S, Riedel J, Herling AW, von Knethen A, Weigert A, Brüne B, Schmoll D. Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling. J Biol Chem. 2015 Nov 20;290(47):28446-55. doi: 10.1074/jbc.M115.678136. Epub 2015 Oct 12. PubMed PMID: 26459563; PubMed Central PMCID: PMC4653701.