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SR1078

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Catalog No. T4594Cas No. 1246525-60-9
Alias SR 1078

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

SR1078

SR1078

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Purity: 99.58%
Catalog No. T4594Alias SR 1078Cas No. 1246525-60-9
SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$35In StockIn Stock
2 mg$50In StockIn Stock
5 mg$82In StockIn Stock
10 mg$117In StockIn Stock
25 mg$238In StockIn Stock
50 mg$387In StockIn Stock
100 mg$575In StockIn Stock
1 mL x 10 mM (in DMSO)$84In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.58%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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].
SynonymsSR 1078
Chemical Properties
Molecular Weight431.25
FormulaC17H10F9NO2
Cas No.1246525-60-9
SmilesOC(c1ccc(NC(=O)c2ccc(cc2)C(F)(F)F)cc1)(C(F)(F)F)C(F)(F)F
Relative Density.1.527 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (104.35 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3188 mL11.5942 mL23.1884 mL115.9420 mL
5 mM0.4638 mL2.3188 mL4.6377 mL23.1884 mL
10 mM0.2319 mL1.1594 mL2.3188 mL11.5942 mL
20 mM0.1159 mL0.5797 mL1.1594 mL5.7971 mL
50 mM0.0464 mL0.2319 mL0.4638 mL2.3188 mL
100 mM0.0232 mL0.1159 mL0.2319 mL1.1594 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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