Potent, selective RORα and RORγt inverse agonist (K i values are 172 and 111 nM for RORα and RORγ respectively). Suppresses IL-17 promoter driven transcriptional activity. Inhibits TRAP220 nuclear receptor box 2 peptide interaction (IC 50 = 117 nM).
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
AGONIST
Mechanism of action
Agonist of RAR-related orphan receptor-α;Agonist of RAR-related orphan receptor-γ
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
SR1001 has been used for inhibiting retinoid-related orphan receptor-γ t (RORγT) activation in Itch−/− mice.
SR1001 has been used as retinoic-acid receptor (RAR)-related orphan nuclear receptor gamma (RORγt) inhibitor to study its effects on interleukin 17 (IL-17) expression in itch cells , as a RAR-related orphan receptor alpha (RORα)- inhibitor to study its effects on RORα-dependent transcription of glucose-6-phosphatase (G6Pase) .
Associated Targets
BRD4Tchem Bromodomain-containing protein 4 0 Activities
1.Solt LA, Kumar N, Nuhant P, Wang Y, Lauer JL, Liu J, Istrate MA, Kamenecka TM, Roush WR, Vidović D et al.. (2011) Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand.. Nature, 472 (7344):(491-4). [PMID:21499262]
2.Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez RD, Burris TP, Griffin PR. (2010) The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist.. Mol Pharmacol, 77 (2):(228-36). [PMID:19887649]
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A2215001