solo para uso en investigación
Cat. No.: S3654
Estructura química
| Dianas relacionadas | HSP JNK Antioxidant ROS eIF IRE1 PERK PDI PKR ASK |
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| Productos destacados | Y-27632 Dihydrochloride SB431542 CHIR-99021 (Laduviglusib) RMC-7977 RMC-6236 (Daraxonrasib) MRTX1133 MG132 Z-VAD-FMK VT3989 IAG933 |
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | PMID |
|---|---|---|---|---|---|---|
| CHO cells | Function assay | Agonist activity at human TGR5 expressed in CHO cells by luciferase assay, EC50=30 μM | 18307294 | |||
| Sf9 | Function assay | TP_TRANSPORTER: uptake in membrane vesicles from Bsep-expressing Sf9 cells, Km=4.1μM | 10648470 | |||
| MDCK | Function assay | TP_TRANSPORTER: uptake in Oatp3-expressing MDCK cells, Km=6.6μM | 11093941 | |||
| HEK293 | Function assay | 90 mins | Inhibition of human ATX expressed in HEK293 Flp-In cells assessed as decrease in choline release from LPC measured every 30 secs for 90 mins by HVA based fluorescence assay, IC50=10.3μM | 28165241 | ||
| Sf9 | Function assay | TP_TRANSPORTER: uptake in membrane vesicles isolated from Bsep-expressing Sf9 cells, Km=11.9μM | 12404240 | |||
| CHO | Function assay | TP_TRANSPORTER: uptake in Ntcp-expressing CHO cells, Km=14μM | 9486191 | |||
| COS | Function assay | TP_TRANSPORTER: inhibition of Taurocholate uptake in ASBT-expressing COS cells, Ki=28μM | 9458785 | |||
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against tunicamycin-induced ER stress in human HuH7 cells assessed as inhibition of CHOP mRNA levels after 6 hrs | 27729186 | ||
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against DCA-induced ER stress in human HuH7 cells assessed as increase in XBPu mRNA levels after 6 hrs | 27729186 | ||
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against tunicamycin-induced ER stress in human HuH7 cells assessed as increase in XBPu mRNA levels after 6 hrs | 27729186 | ||
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against DCA-induced ER stress in human HuH7 cells assessed as inhibition of XBPs mRNA levels after 6 hrs | 27729186 | ||
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against tunicamycin-induced ER stress in human HuH7 cells assessed as inhibition of XBPs mRNA levels after 6 hrs | 27729186 | ||
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against tunicamycin-induced ER stress in human HuH7 cells assessed as reduction in XBPs/XBPu ratio after 6 hrs | 27729186 | ||
| HuH7 | Cytoprotective assay | 1 mM | 24 hrs | Cytoprotective activity against DCA-induced cell death in human HuH7 cells assessed as increase in cell viability at 1 mM preincubated with cells followed by DCA addition measured after 24 hrs by MTT/INCELL assay | 27729186 | |
| HuH7 | Cytoprotective assay | 6 hrs | Cytoprotective activity against tunicamycin-induced ER stress in human HuH7 cells assessed as inhibition of BIP/GRP78 mRNA levels after 6 hrs | 27729186 | ||
| HEK293 | Function assay | Non-competitive inhibition of human ATX expressed in HEK293 Flp-In cells assessed as decrease in LPC hydrolysis by Lineweaver-Burk plot analysis | 28165241 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| Peso molecular | 499.70 | Fórmula | C26H45NO6S |
Almacenamiento (Desde la fecha de recepción) | |
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| Nº CAS | 14605-22-2 | Descargar SDF | Almacenamiento de soluciones madre |
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In vitro |
DMSO
: 100 mg/mL
(200.12 mM)
Water : 100 mg/mL Ethanol : 50 mg/mL |
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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.
| In vitro |
Tauroursodeoxycholic acid (TUDCA) is an endogenous hydrophilic tertiary bile acid produced in humans at a low level. In ER stress conditions, treatment with this compound reduces the activation of ER stress-associated proteins, including GRP78, PERK, eIF2α, ATF4, IRE1α, JNK, p38, and CHOP, and inhibits the dissociation between GRP78 and PERK, resulting in reduced ER stress-mediated cell death. It also increases PrPC (Cellular prion protein) expression. TUDCA regulates stem cell differentiation into various lineages such as adipogenic and osteogenic lineages. It attenuates ER stress, prevents unfolded protein response dysfunction, and stabilizes mitochondria. Under ER stress, treatment with this compound significantly increases the expression of BCL-2 and significantly decreases the expression of Bax, cleaved caspase-3, and cleaved PARP-1, compared with that of untreated cells.
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| In vivo |
Tauroursodeoxycholic Acid (TUDCA) is effective for treating cholestatic liver diseases and also has an ameliorating effect on several diseases, including neurodegenerative diseases, osteoarthritis, vascular diseases, and diabetes. In a murine hindlimb ischemia model, TUDCA-treated mesenchymal stem cells (MSCs) transplantation augments the blood perfusion ratio, vessel formation, and transplanted cell survival more than untreated MSC transplantation does. Augmented functional recovery following MSC transplantation is blocked by PrPC downregulation. Several studies in animals have shown that this compound, an endogenous ambiphilic bile acid, can inhibit unfolded protein response dysfunction and ameliorate ER stress. Its administration attenuates HDM-induced ER stress, airway inflammation, mucus metaplasia, airway remodeling, and methacholine-induced AHR.
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Referencias |
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| Métodos | Biomarcadores | Imágenes | PMID |
|---|---|---|---|
| Western blot | RIPK1 / RIPK3 / p-RIPK1 / p-RIPK3 CHOP / Caspase-12 / Cleaved caspase-12 PrPc p-Akt / Akt |
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29721028 |
| Growth inhibition assay | Cell viability |
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30038553 |
(datos de https://clinicaltrials.gov, actualizado el 2026-04-21)
| Número NCT | Reclutamiento | Condiciones | Patrocinador/Colaboradores | Fecha de inicio | Fases |
|---|---|---|---|---|---|
| NCT07328009 | RECRUITING | Hepato Cellular Carcinoma (HCC) |
Fudan University |
2026-01-19 | PHASE2 |
| NCT06025630 | RECRUITING | Hypertension |
University of North Texas Health Science Center |
2023-08-15 | PHASE1; PHASE2 |
| NCT07457632 | NOT_YET_RECRUITING | Diabetic Macular Edema (DME) |
University of Alabama at Birmingham |
2026-10-01 | PHASE2 |
| NCT07100392 | RECRUITING | Hepatocellular Carcinoma (HCC) |
Fudan University |
2025-08-14 | PHASE2 |
| NCT07064668 | NOT_YET_RECRUITING | Hepatocellular Carcinoma |
Tongji Hospital |
2025-07-30 | PHASE2 |
| NCT07517276 | NOT_YET_RECRUITING | Metabolic Dysfunction-Associated Steatotic Liver Disease Infant Development |
Peking University First Hospital |
2026-04-02 | PHASE2 |