Art. -Nr.: HY-103244

CITCO

3 Cited Publications

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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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Reinheit: 99.60%
CAS. Nr.: 338404-52-7
Formel: C₁₉H₁₂Cl₃N₃OS
Molecular Weight:436.74

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

CITCO Chemical Structure

CAS. Nr.: 338404-52-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CAR, PXR^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
COS-1	EC₅₀	0.51 μM Compound: 1; CITCO	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	[PMID: 27145071]
HEK293	EC₅₀	75 nM Compound: CITCO	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	[PMID: 25305688]
HepG2	EC₅₀	0.02 μM Compound: 1; CITCO	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	[PMID: 27145071]
HepG2	EC₅₀	0.57 μM Compound: CITCO	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	[PMID: 31247375]
HepG2	EC₅₀	0.62 μM Compound: 1; CITCO, DL5045	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	[PMID: 31312405]
HepG2	EC₅₀	0.99 μM Compound: 1; CITCO, DL5045	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	[PMID: 31312405]

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes
Concentration:

1, 2.5, 5, 10, 25, 50 μM
Incubation Time:

48 hours
Result:

Resulted in a dose-dependent inhibition of viable cell count and proliferation.

Cell Cycle Analysis^[1]

Cell Line:

The T98G, U87MG, DB29 and DB33 glioma cells
Concentration:

2.5, 5 μM
Incubation Time:

48 hours
Result:

Induced cell cycle arrest differentially in different BTSCs in culture.

Apoptosis Analysis^[1]

Cell Line:

The T98G, U87MG, DB29 and DB33 glioma cells
Concentration:

2.5, 5 or 10 μM
Incubation Time:

48 hours
Result:

Increased the levels of Annexin V-positive apoptotic cells in dose dependently.

Western Blot Analysis^[1]

Cell Line:

T98G, U87MG, DB29 and DB33 glioma cells
Concentration:

0 to 25 μM
Incubation Time:

48 hours
Result:

The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly.

In Vivo

CITCO (intraperitoneal; on days 22, 24, 26, 30 and 36) with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Six- to eight-week-old male athymic nude mice^[1]
Dosage:

25 or 100 μg
Administration:

Intraperitoneal; on days 22, 24, 26, 30 and 36
Result:

Decreased tumour growth.

Chemical Information

CAS. Nr. 338404-52-7
Appearance Solid
Molecular Weight 436.74
Formel C₁₉H₁₂Cl₃N₃OS
Color White to light yellow
SMILES

ClC1=CC=C(C2=C(/C=N/OCC3=CC=C(Cl)C(Cl)=C3)N4C(SC=C4)=N2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-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

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
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
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2897 mL

11.4485 mL

22.8969 mL

5 mM

0.4579 mL

2.2897 mL

4.5794 mL

10 mM

0.2290 mL

1.1448 mL

2.2897 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chakraborty S, et al. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. Br J Cancer. 2011 Feb 1;104(3):448-59. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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CITCO

Apoptosis Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CITCO

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CITCO

Apoptosis Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CITCO

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CITCO Related Classifications

HY-103244 Related Classifications