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Tauroursodeoxycholic Acid (TUDCA) ER Stress Inhibitor

Cat. No.: S3654

Tauroursodeoxycholic Acid (TUDCA) es el conjugado de taurina del ácido ursodesoxicólico (UDCA) y actúa como un estabilizador mitocondrial y agente antiapoptótico en varios modelos de enfermedades neurodegenerativas, incluyendo la enfermedad de Alzheimer (AD), las enfermedades de Parkinson (PD) y las enfermedades de Huntington (HD).
Tauroursodeoxycholic Acid (TUDCA) ER stress Inhibidor Chemical Structure

Estructura química

Peso molecular: 499.70

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.97%
99.97

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 499.70 Fórmula

C26H45NO6S

Almacenamiento (Desde la fecha de recepción)
Nº CAS 14605-22-2 Descargar SDF Almacenamiento de soluciones madre

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 100 mg/mL (200.12 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 100 mg/mL

Ethanol : 50 mg/mL

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Mecanismo de acción (Mechanism of Action)

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.
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.
Referencias

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes PMID
Western blot RIPK1 / RIPK3 / p-RIPK1 / p-RIPK3 CHOP / Caspase-12 / Cleaved caspase-12 PrPc p-Akt / Akt
S3654-WB4
29721028
Growth inhibition assay Cell viability
S3654-viability1
30038553

Información del ensayo clínico (Clinical Trial Information)

(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