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CITCO CAR agonist

Name: CITCO
Brand: Selleck Chemicals
SKU: S9914
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9914

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.

Chemical Structure

Molecular Weight: 436.74

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

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

99.43

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS
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Chemical Information, Storage & Stability

Molecular Weight	436.74	Formula	C₁₉H₁₂Cl₃N₃OS	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	338404-52-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

In vitro
Batch:

DMSO : 87 mg/mL (199.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CAR ^[1] (in CAR/SRC-1 FRET assay) 49 nM(EC50)
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	[1] https://pubmed.ncbi.nlm.nih.gov/12611900/ [2] https://pubmed.ncbi.nlm.nih.gov/21224854/

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