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.

• Sinonimo/i: RORα/γ Agonist, SR1078, SR1078, N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-4-(trifluoromethyl)benzamide
• Formula empirica (notazione di Hill): C₁₇H₁₀F₉NO₂
• Numero CAS: 1246525-60-9
• Peso molecolare: 431.25
• Numero MDL: MFCD18782737
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥99% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Condizioni di spedizione: wet ice
• Temperatura di conservazione: −20°C
• Stringa SMILE: 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); DUXWIYXHHGNUJU-UHFFFAOYSA-N

Descrizione

Descrizione generale

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).

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
RORα/γ

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Wang, Y., et al. 2010. ACS Chem Biol.5, 1029.
Wang, Y., et al. 2012. PLoS One.7, e34921.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable