Home Metabolism CAR agonist CITCO For research use only.

CITCO

CITCO is a potent and selective constitutive androstane receptor (CAR) agonist with EC50 of 49 nM. CITCO displays >50-fold selectivity for CAR over PXR in the transient transfection assay.

CITCO Chemical Structure

CITCO Chemical Structure

CAS No. 338404-52-7

Purity & Quality Control

Batch: S991401 DMSO]87 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.43%
99.43

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Biological Activity

Description

CITCO is a potent and selective constitutive androstane receptor (CAR) agonist with EC50 of 49 nM. CITCO displays >50-fold selectivity for CAR over PXR in the transient transfection assay.
Targets
CAR [1]
(in CAR/SRC-1 FRET assay)
49 nM(EC50)
In vitro
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. CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes. CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes. CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Cell Research Cell lines Human glioma cell lines, primary human astrocytes
Concentrations 1, 2.5, 5, 10, 25, 50 μM
Incubation Time 48 h
Method

The glioma cells are dissociated using 0.25% trypsin with 0.05 mM EDTA solution and subcultured once in 3–5 days. Primary human astrocytes are cultured in astrocyte medium.Cells are cultured in the absence or presence of CITCO at 37°C for different time points for proliferation assay, cell cycle analysis, apoptosis assay.
In Vivo
In vivo

CITCO with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO. <sup><a class="sref" href="#s_ref">[2]</a></sup>
Animal Research Animal Models Six- to eight-week-old male athymic nude mice
Dosages 25 μg, 100 μg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 436.74 Formula

C19H12Cl3N3OS
CAS No. 338404-52-7 SDF --
Smiles ClC1=CC=C(C=C1)C2=C(\C=N\OCC3=CC=C(Cl)C(=C3)Cl)[N]4C=CSC4=N2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (199.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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