Cilofexor
Based on 10 publication(s) in Google Scholar
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.87%
- No. CAS: 1418274-28-8
- Fòrmula: C28H22Cl3N3O5
- Peso molecular:586.85
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) Cilofexor
More- Science. 2023 Jun 9;380(6649):eabo2296. [Abstract]
- Nat Commun. 2024 May 13;15(1):4034. [Abstract]
- Arch Toxicol. 2022 Jun;96(6):1829-1843. [Abstract]
- JHEP Rep. 2023 Sep 25;6(1):100917. [Abstract]
- Biochem Biophys Res Commun. 2022 Mar 5:595:1-6. [Abstract]
- bioRxiv. 2024 June 11.
- Biomed Pharmacother. 2024 Apr:173:116331. [Abstract]
- bioRxiv. 2024 Feb 8:2023.11.20.567833. [Abstract]
- Université Laval. 2023 Nov 8.
- Patent. US20230310630A1.
Customer Validation & Images
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RT-PCR
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In Vivo Efficacy Study
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Histological Imaging/Staining
Actividad biológica
EC50: 43 nM (FXR)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats received a choline-deficient high fat diet (CDHFD)[3]
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Dosage:30 mg/kg
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Administration:Oral gavage; once daily; for 10 weeks
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Result:Significantly increased Fgf15 expression in the ileum and decreased Cyp7a1 in the liver. Liver fibrosis and hepatic collagen expression were significantly reduced.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1418274-28-8
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Appearance Solid
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Peso molecular 586.85
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Fòrmula C28H22Cl3N3O5
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Color Off-white to light yellow
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SMILES
ClC1=C(C2(CN(C3=CC(C(O)=O)=CC=N3)C2)O)C=CC(OCC4=C(C5CC5)ON=C4C(C(Cl)=CC=C6)=C6Cl)=C1
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Synonyms
GS-9674
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Science
A microbiota-modulated checkpoint directs immunosuppressive intestinal T cells into cancers. [Abstract]2023 Jun 9;380(6649):eabo2296. PMID: 37289890 -
Nat Commun
Mapping of mitogen and metabolic sensitivity in organoids defines requirements for human hepatocyte growth. [Abstract]2024 May 13;15(1):4034. PMID: 38740814 -
Arch Toxicol
Farnesoid X receptor (FXR) agonists induce hepatocellular apoptosis and impair hepatic functions via FXR/SHP pathway. [Abstract]2022 Jun;96(6):1829-1843. PMID: 35267068 -
JHEP Rep
Combined inhibition of bile salt synthesis and intestinal uptake reduces cholestatic liver damage and colonic bile salts in mice. [Abstract]2023 Sep 25;6(1):100917. PMID: 38074508
Cilofexor purchased from MedChemExpress. Usage Cited in: JHEP Rep. 2023 Sep 25;6(1):100917. [Abstract]
Compared with the placebo group, spleen weight was reduced in the cilofexor (30 mg/kg), OCA + ASBTi, and cilofexor + ASBTi treatment groups, indicating a reduction in the inflammatory response in these groups.
Cilofexor purchased from MedChemExpress. Usage Cited in: JHEP Rep. 2023 Sep 25;6(1):100917. [Abstract]
Cilofexor (30 mg/kg). Liver tissues were stained with hematoxylin-eosin (H&E), Sirius Red, CK7, PDGFRβ, α-SMA, COL1A1, and desmin.
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Biochem Biophys Res Commun
Structural insight into the molecular mechanism of cilofexor binding to the farnesoid X receptor. [Abstract]2022 Mar 5:595:1-6. PMID: 35091108 -
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Biomed Pharmacother
Improvement of NASH and liver fibrosis through modulation of the gut-liver axis by a novel intestinal FXR agonist. [Abstract]2024 Apr:173:116331. PMID: 38428307 -
bioRxiv
Hammerhead-type FXR agonists induce an eRNA FincoR that ameliorates nonalcoholic steatohepatitis in mice. [Abstract]2024 Feb 8:2023.11.20.567833. PMID: 38045226
Cilofexor purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Feb 8:2023.11.20.567833. [Abstract]
qPCR data showing FincoR expression levels in C57BL/6 mice liver respectively treated with GW4064 (30 mg/kg), Cilofexor (30 mg/kg), Tropifexor (0.5 mg/kg), Fexaramine (100 mg/kg), or OCA (20 mg/kg) for 1 h (n=3~4/group).
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Solvente y solubilidad
DMSO : 50 mg/mL (85.20 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Trauner M, et al. The Nonsteroidal Farnesoid X Receptor Agonist Cilofexor (GS-9674) Improves Markers of Cholestasis and Liver Injury in Patients With Primary Sclerosing Cholangitis. Hepatology. 2019 Sep;70(3):788-801. [Content Brief]
[2]. Patel K, et al. Cilofexor, a Nonsteroidal FXR Agonist, in Non-Cirrhotic Patients with Nonalcoholic Steatohepatitis: A Phase 2 Randomized Controlled Trial. Hepatology. 2020 Mar 1. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7040 mL | 8.5201 mL | 17.0401 mL | 42.6003 mL |
| 5 mM | 0.3408 mL | 1.7040 mL | 3.4080 mL | 8.5201 mL | |
| 10 mM | 0.1704 mL | 0.8520 mL | 1.7040 mL | 4.2600 mL | |
| 15 mM | 0.1136 mL | 0.5680 mL | 1.1360 mL | 2.8400 mL | |
| 20 mM | 0.0852 mL | 0.4260 mL | 0.8520 mL | 2.1300 mL | |
| 25 mM | 0.0682 mL | 0.3408 mL | 0.6816 mL | 1.7040 mL | |
| 30 mM | 0.0568 mL | 0.2840 mL | 0.5680 mL | 1.4200 mL | |
| 40 mM | 0.0426 mL | 0.2130 mL | 0.4260 mL | 1.0650 mL | |
| 50 mM | 0.0341 mL | 0.1704 mL | 0.3408 mL | 0.8520 mL | |
| 60 mM | 0.0284 mL | 0.1420 mL | 0.2840 mL | 0.7100 mL | |
| 80 mM | 0.0213 mL | 0.1065 mL | 0.2130 mL | 0.5325 mL |
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