557352
RORα/γ Agonist, SR1078
The RORα/γ Agonist, SR1078 controls the biological activity of RORα/γ. This small molecule/inhibitor is primarily used for Biochemicals applications.
Synonym(s):
RORα/γ Agonist, SR1078, SR1078, N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-4-(trifluoromethyl)benzamide
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About This Item
Empirical Formula (Hill Notation):
C17H10F9NO2
CAS Number:
Molecular Weight:
431.25
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥99% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
shipped in
wet ice
storage temp.
−20°C
SMILES string
O=C(NC1=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C1)C2=CC=C(C=C2)C(F)(F)F
InChI
1S/C17H10F9NO2/c18-15(19,20)11-3-1-9(2-4-11)13(28)27-12-7-5-10(6-8-12)14(29,16(21,22)23)17(24,25)26/h1-8,29H,(H,27,28)
InChI key
DUXWIYXHHGNUJU-UHFFFAOYSA-N
General description
A cell-permeable diaryl amide derived from T1317 (a known LXR agonist and retinoic acid receptor (ROR) inverse agonist) that acts as a highly selective agonist of RORα/γ and does not exhibit affinity for FXR, LXRa and LXRb. Shown to stabilize p53 in cancer cells and increase the expression of p21 and PUMA. Induces apoptosis in hepatocellular carcinoma (HepG2) cells in a RORα and p53-dependent process. Also reported to increase the expression of Sox4 and REV-ERBα in HepG2 cells. Exhibits suitable pharmacokinetic properties with sustained plasma levels even after 8 hours following a single i.p. injection. Exposure to SR1078 Induces expression of glucose-6-phosphatase and fibroblast growth factor 21 in murine models (10 mg/kg/i.p).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
RORα/γ
RORα/γ
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wang, Y., et al. 2010. ACS Chem Biol.5, 1029.
Wang, Y., et al. 2012. PLoS One.7, e34921.
Wang, Y., et al. 2012. PLoS One.7, e34921.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Myrthala Moreno-Smith et al.
Nature communications, 12(1), 4006-4006 (2021-06-30)
MYCN activation is a hallmark of advanced neuroblastoma (NB) and a known master regulator of metabolic reprogramming, favoring NB adaptation to its microenvironment. We found that the expression of the main regulators of the molecular clock loops is profoundly disrupted