GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding. It inhibits the expression of IL-17 (at 0.5 uM) in nave CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.
GSK805
Catalog No.: GC18591Purity:>98%
GSK805 es un inhibidor de RORγt activo por vÍa oral y que penetra en el SNC.
Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.
Cas No.: 1426802-50-7
10mM (in 1mL DMSO)In Stock
$158.00
1
1mgIn Stock
$54.00
1
5mgIn Stock
$135.00
1
10mgIn Stock
$216.00
1
25mgIn Stock
$410.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $158.00 | In Stock | 1 | |
| 1mg | $54.00 | In Stock | 1 | |
| 5mg | $135.00 | In Stock | 1 | |
| 10mg | $216.00 | In Stock | 1 | |
| 25mg | $410.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citas (Citations)
Actualmente no hay citas disponibles para este producto. A continuación se muestran publicaciones seleccionadas que citan productos GlpBio.
Nature641, 529–536 (2025)
Nature628, 630–638 (2024)
Nature632, 686–694 (2024)
Nature618, 1017–1023 (2023)
Nature610, 366–372 (2022)
Cell187(9):2288-2304 (2024)
Cell183(7):1867-1883 (2020)
Science388(6745) (2025)
Science387(6739) (2025)
Science387(6734) (2025)
Cell Research35, 97–116 (2025)
Cell Research34, 683–706 (2024)
Cell Research33, 273–287 (2023)
Cell Research33, 546–561 (2023)
Cell Research33, 904–922 (2023)
Cell Research31, 1291–1307 (2021)
Descripción (Description)
Protocolo (Protocol)
Animal experiment: | Animal administration[1]GSK805 are orally administered once daily at 3 doses (1, 3, and 10 mg/kg) to EAE mice from the day of immunization. Compared to the control, the treatment with 9a or 9g resulted in a delay and significant reduction in clinical severity of EAE in a dose-dependent manner. Compared to thiazole ketone amide 2, which only showed EAE efficacy up to day 20 at 100 mg/kg twice daily dosing,32 the biaryl amides 9a and 9g are much more efficacious. This could be attributed to their good in vitro activities as well as much improved oral exposure and CNS penetration. However, it should be noted that although 9g had more brain exposure than 9a, it exhibited less efficacy than 9a in EAE experiments, indicating that there might be additional factors such as "free" brain concentration affecting in vivo efficacy[1]. |
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. | |
Propiedades químicas (Chemical Properties)
N.º CAS
1426802-50-7
Nombre químico
N-[2,6-dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)-benzeneacetamide
SMILES
ClC1=CC(NC(CC2=CC=C(S(CC)(=O)=O)C=C2)=O)=CC(Cl)=C1C3=C(OC(F)(F)F)C=CC=C3
Fórmula molecular
C23H18Cl2F3NO4S
Peso molecular
532.4
Solubilidad
DMF: 3 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.
Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad
g/mol
Reviews
Review for GSK805
Rating: 5
- 5 Star100%
- 4 Star0%
- 3 Star0%
- 2 Star0%
- 1 Star0%