Chenodeoxycholic acid 3-glucuronide
Based on 1 Customer Validation
Chenodeoxycholic acid 3-glucuronide is a derivative of chenodeoxycholic acid (HY-76847). Chenodeoxycholic acid 3-glucuronide activates FXR-dependent transcription, with an EC50 of 8 μM for hFXR. Chenodeoxycholic acid 3-glucuronide upregulates the expression of BSEP, OSTα, and OSTβ transporters. Chenodeoxycholic acid 3-glucuronide accumulates under cholestasis and biliary obstruction conditions, its levels decrease after biliary stent implantation, and it participates in the hepatic detoxification process of chenodeoxycholic acid. Chenodeoxycholic acid 3-glucuronide can be used in the study of cholestasis.
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- Purity : 99.9%
- CAS No.: 58814-71-4
- 화학식: C30H48O10
- 분자량:568.70
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Endogenous Metabolite Isoforms
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Biological Activity
제품 설명
IC50 & Target
[2]|
Human Endogenous Metabolite |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
11 μM
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FXR transactivation activity in transiently transfected HEK293T cells with an FXRE IR-1 firefly luciferase reporter and renilla luciferase normalization vector incubated for 18 h post-stimulation measured by dual luciferase assay.
FXR transactivation activity in transiently transfected HEK293T cells with an FXRE IR-1 firefly luciferase reporter and renilla luciferase normalization vector incubated for 18 h post-stimulation measured by dual luciferase assay.
|
29275233 |
In Vitro
Chenodeoxycholic acid 3-glucuronide binds to hFXR in cell-free coactivator recruitment assays, with an EC50 of 8 μM, and exhibits slightly higher efficacy than CDCA (HY-76847)[1].
Chenodeoxycholic acid 3-glucuronide (1-100 μM; 18 h) activates FXR-dependent transcription in transfected HEK293T cells, with an EC50 of 11 μM[1].
Chenodeoxycholic acid 3-glucuronide (50 μM; 18 h) upregulates the FXR target genes BSEP, OSTα and OSTβ in HepG2 hepatocellular carcinoma cells at a concentration of 50 μM[1].
Chenodeoxycholic acid 3-glucuronide does not regulate the nuclear receptors PXR, LXRα, CAR, or PPAR in cell-free AlphaScreen assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:50 μM
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Incubation Time:18 h
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Result:Positively regulated the expression of BSEP, OSTα, and OSTβ transporter genes at 50 μM.
Showed no apparent effect on MDR1, MDR3, MRP1, MRP2, MRP4, MRP9, and ABCG5/8 gene expression.
Chemical Information
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CAS No. 58814-71-4
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Appearance Solid
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분자량 568.70
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화학식 C30H48O10
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Color White to off-white
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SMILES
C[C@@]12[C@]3([H])[C@]([C@@H](C[C@]1([H])C[C@@H](CC2)O[C@@H]4O[C@@H]([C@H]([C@@H]([C@H]4O)O)O)C(O)=O)O)([H])[C@@]5([H])[C@](CC3)([C@@](CC5)([H])[C@H](C)CCC(O)=O)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 2.5 mg/mL (4.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Mostarda S, et al. Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification. European journal of medicinal chemistry. 2018 Jan 20;144:349-358. [Content Brief]
[2]. Trottier J, et al. Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology. 2006 Nov;44(5):1158-70. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7584 mL | 8.7920 mL | 17.5840 mL | 43.9599 mL |