CH-223191

SKU: orb1225387

Description

CH-223191 is a potent, specific antagonist of AhR (aryl hydrocarbon receptor), potently inhibits TCDD-induced AhR-dependent transcription with IC50 of 0.03 uM; shows more inhibitory potency and no agonist-like effect, compared with flavone, resveratrol, and α-naphthoflavone, as well as estrogenic potency; inhibits TCDD-AhR binding and TCDD-induced nuclear translocation and DNA binding of AhR, prevents the expression of cytochrome P450 enzymes, target genes of the AhR; potently prevents TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice.(In Vitro):CH-223191 (0.1-10 μM; pre-treated 1 hour) inhibits TCDD-caused cytochrome P450 1A1 mRNA expression in a in dose-dependent manner.CH-223191 (0.1-10 μM; pre-treated 1 hour) causes a concentration-dependent inhibition of TCDD-induced cytochrome P450 enzyme activity.(In Vivo):CH-223191 (10 mg/kg; once a day; 25 days) suppresses cytochrome P450 1A1 expression and the intrahepatocyte fat content in liver, reduces activity of AST and ALT in TCDD-treated mice.

Key Properties

• CAS Number: 301326-22-7
• MW: 333.3871
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₉N₅O
• SMILES: O=C(C1=CC=NN1C)NC2=CC=C(/N=N/C3=CC=CC=C3C)C=C2C
• Target: AhR
• Solubility: DMSO: ≥ 35 mg/mL

Bioactivity

• In Vivo:
  CH-223191 (10 mg/kg; once a day; 25 days) suppresses cytochrome P450 1A1 expression and the intrahepatocyte fat content in liver, reduces activity of AST and ALT in TCDD-treated mice. Animal model: Male ICR mice (6 weeks old). Dosage: 10 mg/kg. Administration: 10 mg/kg; once a day; 25 days. Result: Prevented TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice.
• In Vitro:
  CH-223191 (0.1-10 μM; pre-treated 1 hour)inhibits TCDD-causedcytochrome P450 1A1 mRNA expression in a in dose-dependent manner. CH-223191 (0.1-10 μM; pre-treated 1 hour) causes a concentration-dependent inhibition of TCDD-induced cytochrome P450 enzyme activity. RT-PCR Cell line: HepG2 cells. Concentration: 0.1-10 μM Incubation time: 1 hour. Result: Caused inhibition of TCDD-induced cytochrome P450 mRNA expression. Western blot analysis. Cell line: HepG2 cells. Concentration: 0.1-10 μM Incubation time: 1 hour. Result: Decreased TCDD-caused cytochrome P450 1A1 protein Treatment.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CH223191

Quick Database Links

Gene Symbol

AhR