CITCO
Based on 3 publication(s) in Google Scholar
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.
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- Pureza: 99.60%
- No. CAS: 338404-52-7
- Fòrmula: C19H12Cl3N3OS
- Peso molecular:436.74
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CITCO
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Actividad biológica
CAR, PXR[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-1 | EC50 |
0.51 μM
Compound: 1; CITCO
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Agonist activity at human CAR3 expressed in African green monkey COS-1 cells cotransfected with RXRalpha after 24 hrs by CYP2B6-luciferase reporter gene assay
Agonist activity at human CAR3 expressed in African green monkey COS-1 cells cotransfected with RXRalpha after 24 hrs by CYP2B6-luciferase reporter gene assay
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[PMID: 27145071] |
| HEK293 | EC50 |
75 nM
Compound: CITCO
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Agonist activity at human CAR expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human CAR expressed in HEK293 cells by luciferase reporter gene assay
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[PMID: 25305688] |
| HepG2 | EC50 |
0.02 μM
Compound: 1; CITCO
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Agonist activity at CAR LBD (108 to 348 residues) expressed in human HepG2 cells assessed as receptor binding to PGC1alpha by lanthascreenTR-FRET coactivator assay
Agonist activity at CAR LBD (108 to 348 residues) expressed in human HepG2 cells assessed as receptor binding to PGC1alpha by lanthascreenTR-FRET coactivator assay
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[PMID: 27145071] |
| HepG2 | EC50 |
0.57 μM
Compound: CITCO
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Agonist activity at human constitutive androstane receptor expressed in HepG2 cells co-expressing CYP2B6 incubated for 23 hrs by One-Glo luciferase reporter gene assay
Agonist activity at human constitutive androstane receptor expressed in HepG2 cells co-expressing CYP2B6 incubated for 23 hrs by One-Glo luciferase reporter gene assay
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[PMID: 31247375] |
| HepG2 | EC50 |
0.62 μM
Compound: 1; CITCO, DL5045
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Agonist activity at human CAR transfected in human HepG2 cells cotransfected with CYP2B6 incubated for 23 hrs by luciferase reported gene assay
Agonist activity at human CAR transfected in human HepG2 cells cotransfected with CYP2B6 incubated for 23 hrs by luciferase reported gene assay
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[PMID: 31312405] |
| HepG2 | EC50 |
0.99 μM
Compound: 1; CITCO, DL5045
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Agonist activity at human PXR transfected in human HepG2 cells cotransfected with CYP3A4 incubated for 23 hrs by luciferase reporter gene assay
Agonist activity at human PXR transfected in human HepG2 cells cotransfected with CYP3A4 incubated for 23 hrs by luciferase reporter gene assay
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[PMID: 31312405] |
CITCO (1-50 μM; 48 hours) results in a dose-dependent inhibition of viable cell count and proliferation in both T98G and U87MG glioma and BTSCs[1].
CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes[1].
CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes[1].
CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein that increased significantly[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes
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Concentration:1, 2.5, 5, 10, 25, 50 μM
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Incubation Time:48 hours
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Result:Resulted in a dose-dependent inhibition of viable cell count and proliferation.
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Cell Line:The T98G, U87MG, DB29 and DB33 glioma cells
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Concentration:2.5, 5 μM
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Incubation Time:48 hours
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Result:Induced cell cycle arrest differentially in different BTSCs in culture.
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Cell Line:The T98G, U87MG, DB29 and DB33 glioma cells
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Concentration:2.5, 5 or 10 μM
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Incubation Time:48 hours
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Result:Increased the levels of Annexin V-positive apoptotic cells in dose dependently.
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Cell Line:T98G, U87MG, DB29 and DB33 glioma cells
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Concentration:0 to 25 μM
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Incubation Time:48 hours
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Result:The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six- to eight-week-old male athymic nude mice[1]
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Dosage:25 or 100 μg
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Administration:Intraperitoneal; on days 22, 24, 26, 30 and 36
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Result:Decreased tumour growth.
Chemical Information
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No. CAS 338404-52-7
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Appearance Solid
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Peso molecular 436.74
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Fòrmula C19H12Cl3N3OS
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Color White to light yellow
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SMILES
ClC1=CC=C(C2=C(/C=N/OCC3=CC=C(Cl)C(Cl)=C3)N4C(SC=C4)=N2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Metab
Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury. [Abstract]2024 Nov 5;36(11):2402-2418.e10. PMID: 39389061 -
Drug Metab Dispos
Switch/sucrose non-fermentable complex interacts with constitutive androstane receptor to regulate drug-metabolizing enzymes and transporters in the liver. [Abstract]2025 Apr;53(4):100057. PMID: 40158296 -
Stem Cells
The effect of Vitamin D3 and Valproic Acid on the maturation of human induced pluripotent stem cell-derived enterocyte-like cells. [Abstract]2023 Aug 16;41(8):775-791. PMID: 37228023
Solvente y solubilidad
DMSO : 25 mg/mL (57.24 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (284 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
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 (sealed storage, away from moisture). 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 | 2.2897 mL | 11.4485 mL | 22.8969 mL | 57.2423 mL |
| 5 mM | 0.4579 mL | 2.2897 mL | 4.5794 mL | 11.4485 mL | |
| 10 mM | 0.2290 mL | 1.1448 mL | 2.2897 mL | 5.7242 mL | |
| 15 mM | 0.1526 mL | 0.7632 mL | 1.5265 mL | 3.8162 mL | |
| 20 mM | 0.1145 mL | 0.5724 mL | 1.1448 mL | 2.8621 mL | |
| 25 mM | 0.0916 mL | 0.4579 mL | 0.9159 mL | 2.2897 mL | |
| 30 mM | 0.0763 mL | 0.3816 mL | 0.7632 mL | 1.9081 mL | |
| 40 mM | 0.0572 mL | 0.2862 mL | 0.5724 mL | 1.4311 mL | |
| 50 mM | 0.0458 mL | 0.2290 mL | 0.4579 mL | 1.1448 mL |
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