Product Details
| Product Name:
GSK805 |
CAS No.:
1426802-50-7 |
| Purity:
≥95% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | GSK805 |
| Description | GSK805 is a potent, orally bioavailable and CNS-penetrant RORγt inhibitor. |
| Cell Research | CD4+CD62LhighCD25? naive CD4+ T cells were purified by FACS sorting following a MACS bead isolation of CD4+ cells. Naive CD4+ cells were activated with plate-bound anti-CD3 (2 μg/ml) and anti-CD28 (2 μg/ml). For Th17 cell differentiation, cultures were supplemented with IL-6 (20 ng/ml) plus TGF-β1 (1 ng/ml), and IL-23 (10 ng/ml) was added after 48 h. RORγt inhibitors or vehicle control DMSO was also included in the cultures. After 96 h, cells were collected for further experiments[1]. |
| In vitro | METHODS: CD4 T cells (activated under Th17 cell differentiation conditions) were treated with GSK805 (0.5 μM, 4 days). IL-17 and IFNγ production was measured by intracellular cytokine staining.
RESULTS GSK805 exerted an inhibitory effect on Th17 cell differentiation. [1] |
| In vivo | METHODS: C57BL/6 mice were induced to develop EAE and treated with GSK805 (30 mg/kg, p.o., 14 days). CNS-infiltrating cells were isolated, and IL-17 and IFNγ production was measured by intracellular staining.
RESULTS GSK805 strongly inhibited Th17 cell responses in the CNS (reduced IFNγIL-17 and IFNγIL-17 T cells), whereas the frequency of TNF-α T cells was not significantly altered). [1]
METHODS: GSK805 (1, 3 and 10 mg/kg, orally, three times a day) was administered to EAE mice to observe its effects on the mice.
RESULTS GSK805 can reduce the clinical severity of EAE in a dose-dependent manner. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (18.78 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 100 mg/mL (187.84 mM)
|
| Keywords | GSK 805 | immunity | RAR-related orphan receptor | Inhibitor | inhibit | ROR | oral | CNS penetrant | Th17 cell | GSK-805 | GSK805 |
| Inhibitors Related | S18-000003 | T0901317 | GSK2981278 | Nobiletin | XY101 | Cholesterol | AZD-0284 | Melatonin | SR2211 | Cabozantinib hydrochloride | RORγt Inverse agonist 6 | ML 209 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | CNS-Penetrant Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Transcription Factor-Targeted 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 |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States