SR1078

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

SR1078

CAS No. : 1246525-60-9

MCE 国际站：SR1078

产品活性：SR1078 是一种视黄酸受体相关孤儿受体 (RORα/RORγ) 激动剂。SR1078 直接与 RORα 和 RORγ 的配体结合区结合，提高了这些受体的转录活性，从而刺激了 RORα/γ 靶基因的转录。

研究领域：Metabolic Enzyme/Protease  |  Vitamin D Related/Nuclear Receptor

作用靶点：ROR

In Vitro: 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.
?SR1078 (2-10 μM; 24 hours) shows a dose-dependent increase in expression of A2BP1, CYP19A1, NLGN1, and IPTR1 in SH-SY5Y cells. EC50’s are in the range of 3-5 μM.

In Vivo: 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.
?SR1078 (10 mg/kg; i.p.) shows a significant 25% reduction in repetitive grooming behavior in the BTBR mice.

相关产品：Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Transcription Factor-Targeted Library  |  Nuclear Receptor Compound Library  |  Highly Selective Activators Library  |  T0901317  |  Nobiletin  |  3-Oxo-5β-cholanoic acid  |  SR3335  |  GSK805  |  SR1001  |  Zilovertamab  |  Cintirorgon  |  SR2211  |  XY018  |  GSK2981278  |  Neoruscogenin  |  PF-06747711  |  SR0987  |  TMP920  |  Cedirogant  |  AZD-0284  |  GNE-6468  |  JNJ-61803534  |  RORγt inverse agonist 13  |  TMP778  |  7ß,27-Dihydroxycholesterol  |  GNE-0946  |  S18-000003  |  Vimirogant hydrochloride  |  XY101  |  Bevurogant  |  MRL-871  |  RORγt agonist 3  |  RORγt Inverse agonist 10

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds