- SR3335
| SR1078Orphan receptor agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.32%
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Chemical structure
| Description | SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR) RORα and RORγ with IC50 values of both 1-3 µM. | |||||
| Targets | RORα | RORγ | ||||
| IC50 | 1-3 µM | 1-3 µM | ||||
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| Cas No. | 1246525-60-9 | SDF | Download SDF |
| Synonyms | SR 1078;SR-1078 | ||
| Chemical Name | N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-(trifluoromethyl)benzamide | ||
| Canonical SMILES | C1=CC(=CC=C1C(=O)NC2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O)C(F)(F)F | ||
| Formula | C17H10F9NO2 | M.Wt | 431.25 |
| Solubility | ≥43.2 mg/mL in DMSO, ≥43.4 mg/mL in EtOH, <2.17 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR) RORα and RORγ with IC50 values of both 1-3 µM [1].
RORα and RORγ are two members of nuclear receptor superfamily, which possesses a highly conserved DNA-binding and a ligand-binding domain. These two receptors are considered to play important roles in the regulation of metabolism and the function of immune system [1].
SR1078 is a selective RORα and RORγ agonist, which activate RORα and RORγ directed transcription via inducing conformational changes [1].
SR1078 selectively targets on RORα and RORγ as an agonist but not on LXR and FXR [1]. It was shown that SR1078 was able to stimulate ROR activity and subsequent ROR-directed mRNA expression. When HepG2 cells were treated with SR1078 for 24h, the ROR directed reporter gene FG21 mRNA level was increased by 3-fold, while another reporter gene G6Pase was increased by 2-fold [1].
In mouse model, i.p. injection of 10 mg/kg SR1078 for 1 hr resulted in 3.6 μM plasma concentration., and after 8 hr the concentration still sustained at 800 nM. i.p. injection of 10 mg/kg SR1078 for 2 hr resulted in significantly increased level of mRNA of reporter gene G6Pase and FG21 [1].
Reference:[1] Wang Y et al. , Identification of a Synthetic Agonist for the Orphan Nuclear Receptors RORα and RORγ, SR1078. ACS Chem Biol., 2010, 5(11): 1029-1034.
