GSK805
Based on 5 publication(s) in Google Scholar
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.
- Purity: 99.83%
- CAS No.: 1426802-50-7
- Formula: C23H18Cl2F3NO4S
- Molecular Weight:532.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK805
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Customer Validation & Images
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Microbiological Assay
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Flow Cytometry
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Bio/Physico-chemical Assay
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Histological Imaging/Staining
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Flow Cytometry
Biological Activity
IC50: 8.4 (RORγt)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
13.32 μM
Compound: 2; GSK805
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Antiproliferative activity against human 22Rv1 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human 22Rv1 cells incubated for 4 days by CCK8 assay
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[PMID: 38227771] |
| LNCaP | IC50 |
7.68 μM
Compound: 2; GSK805
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Antiproliferative activity against human LNCaP cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human LNCaP cells incubated for 4 days by CCK8 assay
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[PMID: 38227771] |
| LNCaP C4-2B | IC50 |
5.82 μM
Compound: 2; GSK805
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Antiproliferative activity against human LNCaP C4-2B cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human LNCaP C4-2B cells incubated for 4 days by CCK8 assay
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[PMID: 38227771] |
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.
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Cell Line:CD4+ T cells
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Concentration:0.5 μM
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Incubation Time:4 days
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Result:Inhibited IL-17 production during Th17 cell differentiation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice were immunized with MOG35–55 plus CFA[2]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg once per day; for 35 days
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Result:Efficiently ameliorated the severity of EAE in mice.
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Animal Model:C57BL/6 mice with EAE[2]
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Dosage:30 mg/kg
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Administration:Oral gavage
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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.
Chemical Information
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CAS No. 1426802-50-7
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Appearance Solid
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Molecular Weight 532.36
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Formula C23H18Cl2F3NO4S
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Microbiol
Gut pathobionts underlie intestinal barrier dysfunction and liver T helper 17 cell immune response in primary sclerosing cholangitis. [Abstract]2019 Mar;4(3):492-503. PMID: 30643240
GSK805 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2019 Mar;4(3):492-503. [Abstract]
GSK805 (a ROR-γt inverse agonist (RIA), 10 mg/kg; p.o.; once daily for 14 days). Serum TB (left) and ALP (right) levels of mice.
GSK805 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2019 Mar;4(3):492-503. [Abstract]
GSK805 (a ROR-γt inverse agonist (RIA), 10 mg/kg; p.o.; once daily for 14 days). Representative photomicrographs of Sirius Red staining (upper) and Masson trichrome staining (lower) of the liver sections of mice. Scale bars, 100 µm.
GSK805 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2019 Mar;4(3):492-503. [Abstract]
GSK805 (a ROR-γt inverse agonist (RIA), 10 mg/kg; p.o.; once daily for 14 days). Representative intracellular ROR-γ t and IL-17 staining (upper) and ROR-γ t and IFN-γ staining (lower) of TCR-β+CD4+-gated cells in the liver of mice.
GSK805 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2019 Mar;4(3):492-503. [Abstract]
GSK805 (a ROR-γt inverse agonist (RIA), 10 mg/kg; p.o.; once daily for 14 days). qRT–PCR analysis of Col1a1 (left) and Timp1 (right) relative to Gapdh in the whole liver of mice.
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Adv Sci (Weinh)
Gut Microbiota-Derived Hyocholic Acid Enhances Type 3 Immunity and Protects Against Salmonella enterica Serovar Typhimurium in Neonatal Rats. [Abstract]2025 Mar;12(10):e2412071. PMID: 39737849
GSK805 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(10):e2412071. [Abstract]
STM burden in the rat ileum in the PBS + STM, HCA + STM, and HCA + GSK805 (20 mg/kg; p.o.; once daily for 14 days) + STM groups at 1 dpi, n = 6.
GSK805 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(10):e2412071. [Abstract]
GSK805 (20 mg/kg; p.o.; once daily for 14 days). Representative FACS plots and percentages of γδT cells, IL-17A+γδT cells, ILC3s, and IL-17A+ILC3s in small intestine LPLs, n = 6.
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Proc Natl Acad Sci U S A
2021 Nov 16;118(46):e2105950118. PMID: 34772808 -
Microbiol Res
ScRNA-seq reveals trained immunity-engaged Th17 cell activation against Edwardsiella piscicida-induced intestinal inflammation in teleost. [Abstract]2024 Dec:289:127912. PMID: 39326350 -
Exp Eye Res
2025 Nov:260:110573. PMID: 40819785
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang Y, et al. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors. ACS Med Chem Lett. 2015 May 26;6(7):787-792. [Content Brief]
[2]. Xiao S, et al. Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms. Immunity. 2014 Apr 17;40(4):477-89. [Content Brief]
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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