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SR1078
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SR1078图片
CAS NO:1246525-60-9
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
SR 1078
产品介绍
SR1078 是视黄酸受体相关孤儿受体 (RORα/RORγ) 激动剂。它能够与 RORα 和 RORγ 的配体结合区直接结合,增强该受体的转录活性,促使 RORα/γ 靶基因的转录。

产品描述

SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.

体外活性

SR1078 is a synthetic RORα/RORγ ligand. SR1078 modulates the conformation of RORγ in a biochemical assay and activates RORα and RORγ driven transcription. Furthermore, SR1078 stimulates expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR1078 significantly inhibits the constitutive transactivation activity of RORα and RORγ, but has no effect on the activity of FXR, LXRα and LXRβ. In a RORα cotransfection assay, treatment of cells with SR1078 (10 μM) results in a significant increase in transcription. Similarly, in the RORγ cotransfection assay, SR1078 treatment results in a stimulation of RORγ-dependent transcription activity[1].

体内活性

The pharmacokinetic properties of SR1078 are examined in mice and noted significant exposure. Plasma concentrations reach 3.6 μM 1h after a 10 mg/kg i.p. injection of SR1078 and sustained levels of above 800 nM even 8h after the single injection. These levels are sufficient to perform a proof-of-principle experiment to determine if SR1078 treatment would stimulate ROR target gene expression in an animal model. Mice are treated with SR1078 (10 mg/kg i.p.) and 2h after the injection the livers are harvested and mRNA purified for assessment of?G6Pase?and?FGF21?gene expression.T he expression of both?FGF21?and?G6Pase?is significantly stimulated by SR1078 treatment vs. vehicle control[1].

Cas No.

1246525-60-9

分子式

C17H10F9NO2

分子量

431.25

别名

SR 1078

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years