CITCO is a potent and selective constitutive androstane receptor (CAR) agonist with EC50 of 49 nM. This compound displays >50-fold selectivity for CAR over PXR in the transient transfection assay.
research use only
CITCO CAR agonist
Cat.No.S9914
Chemical Structure
Molecular Weight: 436.74
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| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Other CAR Inhibitors | TCPOBOP |
Chemical Information, Storage & Stability
| Molecular Weight | 436.74 | Formula | C19H12Cl3N3OS |
Storage (From the date of receipt) | 3 years -20°C powder |
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| CAS No. | 338404-52-7 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | ClC1=CC=C(C=C1)C2=C(\C=N\OCC3=CC=C(Cl)C(=C3)Cl)[N]4C=CSC4=N2 | ||
Solubility
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In vitro |
DMSO
: 87 mg/mL
(199.2 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Mechanism of Action
| Targets/IC50/Ki |
CAR
(in CAR/SRC-1 FRET assay) 49 nM(EC50)
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|---|---|
| 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. This compound (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes. It (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes. This chemical (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> |
| 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 of this compound. <sup><a class="sref" href="#s_ref">[2]</a></sup> |
References |
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