CH-223191 AhR antagonist

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Quality Control

Batch: Purity: 99.75%

99.75

Products Often Used Together with CH-223191

PD 98059

It and PD98059 abolish TCDD-induced ERK1/2 phosphorylation and cell proliferation in human colon cancer cells.

FICZ

It is intraperitoneally administered 1 hr before FICZ application to modulate AhR activation.

GNF351

It and GNF351 are AhR antagonists that completely inhibit the VRCZ-induced transcription of CYP1A1 and COX-2 in HaCaT cells.

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other AhR Inhibitors	BAY 2416964 Stemregenin 1 (SR1) BAY-218 Tapinarof Diosmin Norisoboldine L-Kynurenine PDM2 CAY10465 Perillaldehyde

Chemical Information, Storage & Stability

Molecular Weight	333.39	Formula	C₁₉H₁₉N₅O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	301326-22-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC=CC=C1N=NC2=CC(=C(C=C2)NC(=O)C3=CC=NN3C)C

Solubility

In vitro
Batch:

DMSO : 67 mg/mL (200.96 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.850mg/ml (2.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 17 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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.
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.
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	AhR (in HepG2 cells) 30 nM
In vitro	CH-223191 blocks TCDD-mediated nuclear translocation and DNA binding of AhR, and also causes the inhibition of TCDD-induced cytochrome P450 enzyme activity. In human glioblastoma cells, this compound downregulates the TGF-beta/Smad pathway, and reduces clonogenic survival and invasiveness. In SK-N-SH human-derived neuronal cells, this chemical counteracts the TCDD-induced suppression of neuronal acetylcholinesterase expression. In endothelial cells, it potentiates ICAM-1 expression and prevents RelB nuclear translocation.
Kinase Assay	Luciferase Reporter Gene Assay
Kinase Assay	The cells are lysed with lysis buffer (20 mM Tris-HCl, pH 7.8, 1% Triton X-100, 150 mM NaCl, and 2 mM dithiothreitol). The cell lysate is mixed with luciferase activity assay reagent and luminescence produced for 5 s is measured using a luminometer.
In vivo	CH-223191 (10 mg/kg/day, p.o.) potently prevents TCDD-caused cytochrome P450 induction, liver toxicity, and wasting syndrome in mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16540597/ [2] https://pubmed.ncbi.nlm.nih.gov/19465936/ [3] https://pubmed.ncbi.nlm.nih.gov/23426015/ [4] https://pubmed.ncbi.nlm.nih.gov/24752502/

Applications

Methods	Biomarkers	Images	PMID
Western blot	hpol κ / γH2AX		26651356

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Handling Instructions

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Chemical Structure

Molecular Weight: 333.39