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RORγt Inverse agonist 8

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Catalog No. T12754Cas No. 2079892-79-6

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist (human RORγt-LBD) with an IC50 of 19 nM.

RORγt Inverse agonist 8

RORγt Inverse agonist 8

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Catalog No. T12754Cas No. 2079892-79-6
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist (human RORγt-LBD) with an IC50 of 19 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,6706-8 weeks6-8 weeks
50 mg$2,1806-8 weeks6-8 weeks
100 mg$2,8006-8 weeks6-8 weeks
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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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Product Introduction

Bioactivity
Description
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist (human RORγt-LBD) with an IC50 of 19 nM.
Targets&IC50
RORγt:19 nM
In vitro
RORγt Inverse agonist 8 is a potent inhibitor of RORγt and binds to the ligand binding domain (LBD) of RORγt. RORγt Inverse agonist 8 results in complete attenuation of IL-17A secretion in a concentration-dependent manner (IC50 of 60 nM in HUT78 cells). RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation. RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion.
In vivo
antigen-induced arthritis (AiA) responses in Lewis rats ameliorated by RORγt Inverse agonist 8.
Chemical Properties
Molecular Weight475.59
FormulaC26H33N7O2
Cas No.2079892-79-6
SmilesC(C=1C=2N(C=C(NC(=O)C=3C=NC(C)=NC3)C1C)C=CN2)N4C[C@H](C)N(C(=O)C5CCCC5)CC4
Relative Density.1.35 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

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

Keywords

RORγt Inverse agonist 8RORγtRORrt Inverse agonist 8RORgammat Inverse agonist 8
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