solo para uso en investigación
Cat. No.S7904
| Dianas relacionadas | PD-1/PD-L1 CXCR AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor |
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| Otros STING Inhibidores | H-151 C-176 CCCP STING inhibitor C-178 MSA-2 C-171 SN-011 G10 (STING agonist-1) SN-001 Cridanimod |
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | PMID |
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| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.02 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human wild-type STING expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.02 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.04 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.05 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype R232H mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.07 μM. | 31715099 | ||
| 293T | Function assay | 7 hrs | Activation of recombinant human wild-type STING expressed in 293T cells incubated for 7 hrs in absence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 13.7 μM. | 31715099 | ||
| THP1 | Function assay | 20 hrs | Agonist activity at STING in human THP1 cells assessed as stimulation of IRF3 pathway measured after 20 hrs by luciferase reporter gene assay, EC50 = 38.6 μM. | 31820985 | ||
| PBMC | Function assay | 69.6 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in CXCL10 mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis | 31820985 | |
| PBMC | Function assay | 1.39 to 139 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IFNbeta release at 1.39 to 139 uM measured after 4 hrs by ELISA | 31820985 | |
| PBMC | Function assay | 69.6 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IFNbeta mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis | 31820985 | |
| PBMC | Function assay | 69.6 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IL6 mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis | 31820985 | |
| PBMC | Function assay | 139 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IL6 production at 139 uM measured after 4 hrs by ELISA | 31820985 | |
| B16-OVA | Antitumor assay | Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as tumour regression in injected flank at 10 ug administered intratumorally on day 6, 9 and 12 post implantation | 31500996 | |||
| B16-OVA | Antitumor assay | Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as tumour regression in contralateral flank at 10 ug administered intratumorally on day 6, 9 and 12 post implantation | 31500996 | |||
| B16-OVA | Antitumor assay | Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as higher number of mouse cured of tumors at 10 ug administered intratumorally on day 6, 9 and 12 post implantation | 31500996 | |||
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| Peso molecular | 718.37 | Fórmula | C20H22N10Na2O13P2 |
Almacenamiento (Desde la fecha de recepción) | 3 years -20°C powder |
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| Nº CAS | 2734858-36-5 | -- | Almacenamiento de soluciones madre |
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In vitro |
DMSO
: 100 mg/mL
(139.2 mM)
Water : 100 mg/mL Ethanol : Insoluble |
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In vivo |
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Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)
Resultados del cálculo:
Concentración de trabajo: mg/ml;
Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.
Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.
| Targets/IC50/Ki |
STING
(Cell-free assay) 3.79 nM(Kd)
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| In vitro |
El 2',3'-cGAMP es un segundo mensajero endógeno producido por células de mamíferos. El 2',3'-cGAMP es un ligando de alta afinidad para STING. El 2',3'-cGAMP es un potente inductor de interferones de tipo I. La unión del 2',3'-cGAMP induce cambios conformacionales de STING. |
Referencias |
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