2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. GSK805

GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity.

For research use only. We do not sell to patients.

GSK805 Chemical Structure

GSK805 Chemical Structure

CAS No. : 1426802-50-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 176 In-stock
Solution
10 mM * 1 mL in DMSO USD 176 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 240 In-stock
25 mg USD 480 In-stock
50 mg USD 770 In-stock
100 mg USD 1300 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

GSK805 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity[1].

IC50 & Target

IC50: 8.4 (RORγt)[1]
In Vitro

GSK805 (0.5 μM; 4 d) inhibits Th17 cell responses[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK805 Related Antibodies

Cell Differentiation Assay[2]

Cell Line: CD4+ T cells
Concentration: 0.5 μM
Incubation Time: 4 days
Result: Inhibited IL-17 production during Th17 cell differentiation.
In Vivo

GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE)[2].
GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice were immunized with MOG35–55 plus CFA[2]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg once per day; for 35 days
Result: Efficiently ameliorated the severity of EAE in mice.
Animal Model: C57BL/6 mice with EAE[2]
Dosage: 30 mg/kg
Administration: Oral gavage; 30 mg/kg once
Result: Reduced both IFN-γ-IL-17+ and IFN-γ+IL-17+ T cells without altered the frequency of TNF-α+ T cells in EAE mice.
Molecular Weight

532.36

Formula

C23H18Cl2F3NO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(Cl)=C(C2=CC=CC=C2OC(F)(F)F)C(Cl)=C1)CC3=CC=C(S(=O)(CC)=O)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (187.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8784 mL 9.3921 mL 18.7843 mL
5 mM 0.3757 mL 1.8784 mL 3.7569 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8784 mL 9.3921 mL 18.7843 mL 46.9607 mL
5 mM 0.3757 mL 1.8784 mL 3.7569 mL 9.3921 mL
10 mM 0.1878 mL 0.9392 mL 1.8784 mL 4.6961 mL
15 mM 0.1252 mL 0.6261 mL 1.2523 mL 3.1307 mL
20 mM 0.0939 mL 0.4696 mL 0.9392 mL 2.3480 mL
25 mM 0.0751 mL 0.3757 mL 0.7514 mL 1.8784 mL
30 mM 0.0626 mL 0.3131 mL 0.6261 mL 1.5654 mL
40 mM 0.0470 mL 0.2348 mL 0.4696 mL 1.1740 mL
50 mM 0.0376 mL 0.1878 mL 0.3757 mL 0.9392 mL
60 mM 0.0313 mL 0.1565 mL 0.3131 mL 0.7827 mL
80 mM 0.0235 mL 0.1174 mL 0.2348 mL 0.5870 mL
100 mM 0.0188 mL 0.0939 mL 0.1878 mL 0.4696 mL
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GSK805 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK8051426802-50-7GSK 805GSK-805RORRAR-related orphan receptororalCNS penetrantTh17 cellimmunityInhibitorinhibitorinhibit

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