Product Details
| Product Name:
SR1078 |
CAS No.:
1246525-60-9 |
| Purity:
98.74% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | SR1078 |
| Description | SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ. |
| In vitro | SR1078 is a synthetic RORα/RORγ ligand that modulates the conformation of RORγ in biochemical assays and activates RORα and RORγ-driven transcription. It stimulates the expression of endogenous ROR target genes in HepG2 cells expressing 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, without affecting FXR, LXRα, or LXRβ. Treatment of cells with SR1078 (10 μM) in a RORα cotransfection assay significantly increases transcription, and similarly, in a RORγ cotransfection assay, SR1078 stimulates RORγ-dependent transcription activity[1]. |
| In vivo | The pharmacokinetics of SR1078 were evaluated in mice, revealing notable exposure. Plasma concentrations reached 3.6 μM one hour post 10 mg/kg i.p. injection and remained above 800 nM at 8 hours. These levels are adequate for proof-of-principle experiments assessing ROR target gene expression. Mice treated with SR1078 (10 mg/kg i.p.) showed significant stimulation of both G6Pase and FGF21 gene expression in liver mRNA, compared to vehicle control [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (104.35 mM)
|
| Keywords | inhibit | SR1078 | SR-1078 | ROR | RAR-related orphan receptor | Inhibitor |
| Inhibitors Related | S18-000003 | T0901317 | GSK2981278 | Nobiletin | XY101 | Cholesterol | AZD-0284 | Melatonin | SR2211 | Cabozantinib hydrochloride | RORγt Inverse agonist 6 | ML 209 |
| Related Compound Libraries | Nuclear Receptor Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$1.00/1KG |
VIP6Y
|
Career Henan Chemical Co
|
2019-12-17 |
United States