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557352

RORα/γ Agonist, SR1078

Name: RORα/γ Agonist, SR1078
Brand: MM

The RORα/γ Agonist, SR1078 controls the biological activity of RORα/γ. This small molecule/inhibitor is primarily used for Biochemicals applications.

别名:

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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关于此项目

经验公式（希尔记法）:

C₁₇H₁₀F₉NO₂

化学文摘社编号:

1246525-60-9

分子量:

431.25

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD18782737

Assay:

≥99% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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属性

Quality Segment

100

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

说明

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

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c