endast för forskning
Kat.nr.: S3654
Kemisk struktur
| Relaterade mål | HSP JNK Antioxidant ROS eIF IRE1 PERK PDI PKR ASK |
|---|---|
| Utvalda produkter | Y-27632 Dihydrochloride SB431542 CHIR-99021 (Laduviglusib) RMC-7977 RMC-6236 (Daraxonrasib) MRTX1133 MG132 Z-VAD-FMK VT3989 IAG933 |
| Cellinjer | Analystyp | Koncentration | Inkubationstid | Formulering | Aktivitetsbeskrivning | 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 | |||
| Klicka för att visa mer experimentella data för cellinjer | ||||||
| Molekylvikt | 499.70 | Formel | C26H45NO6S |
Lagring (från mottagningsdatumet) | |
|---|---|---|---|---|---|
| CAS-nr | 14605-22-2 | Ladda ner SDF | Lagring av stamlösningar |
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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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Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)
Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)
Beräkningsresultat:
Arbetskoncentration: mg/ml;
Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )
Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH2O, blanda och klarna.
Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.
Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.
| 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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Referenser |
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| Metoder | Biomarkörer | Bilder | 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 |
(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)
| NCT-nummer | Rekrytering | Tillstånd | Sponsor/Samarbetspartners | Startdatum | Faser |
|---|---|---|---|---|---|
| NCT05753852 | Recruiting | Amyotrophic Lateral Sclerosis |
Humanitas Mirasole SpA|University of Ulm|University of Sheffield|University Hospital Tours|KU Leuven|UMC Utrecht|University of Dublin Trinity College|Bruschettini S.r.l.|Istituto Superiore di Sanità|Motor Neurone Disease Association |
October 25 2021 | Phase 3 |
| NCT04114292 | Unknown status | Ulcerative Colitis |
Washington University School of Medicine|Crohn''s and Colitis Foundation |
January 17 2019 | Phase 1 |
| NCT01899703 | Completed | Cholestasis Intrahepatic |
GlaxoSmithKline |
March 10 2014 | Phase 2 |