| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: =100%
CH-223191 (CH 223191; CH223191) is a potent and specific/selective aryl hydrocarbon receptor (AhR) antagonist with important biological activity. It inhibits AhR with an IC50 of 30 nM. It can prevent 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor. In addition, CH-223191 blocked the binding of TCDD to AhR and inhibited TCDD-mediated nuclear translocation and DNA binding of AhR. These inhibitory effects of CH-223191 prevented the expression of cytochrome P450 enzymes, target genes of the AhR.
| Targets |
AhR (aryl hydrocarbon receptor)
|
|---|---|
| ln Vitro |
In a dose-dependent way, CH-223191 (0.1-10 μM; pre-treated for 1 hour) suppresses the expression of cytochrome P450 1A1 mRNA produced by TCDD[1]. The cytochrome P450 enzyme activity produced by TCDD is inhibited in a concentration-dependent manner by CH-223191 (0.1-10 μM; pre-treated for 1 hour)[1].
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| ln Vivo |
In mice treated with TCDD, CH-223191 (10 mg/kg; once daily; 25 days) decreases the activity of AST and ALT and lowers the expression of cytochrome P450 1A1 and the intrahepatocyte fat content in the liver[1].
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| Enzyme Assay |
In this study, by screening a chemical library composed of approximately 10,000 compounds, we identified a novel compound, 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191), that potently inhibits TCDD-induced AhR-dependent transcription. In addition, CH-223191 blocked the binding of TCDD to AhR and inhibited TCDD-mediated nuclear translocation and DNA binding of AhR. These inhibitory effects of CH-223191 prevented the expression of cytochrome P450 enzymes, target genes of the AhR. Unlike many known antagonists of AhR, CH-223191 did not have detectable AhR agonist-like activity or estrogenic potency, suggesting that CH-223191 is a specific antagonist of AhR[1].
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| Cell Assay |
RT-PCR[1]
Cell Types: HepG2 cells Tested Concentrations: 0.1-10 μM Incubation Duration: 1 hour Experimental Results: Caused inhibition of TCDD-induced cytochrome P450 mRNA expression. Western Blot Analysis[1] Cell Types: HepG2 cells Tested Concentrations: 0.1-10 μM Incubation Duration: 1 hour Experimental Results: diminished TCDD-caused cytochrome P450 1A1 protein Treatment. |
| Animal Protocol |
Animal/Disease Models: Male ICR mice (6 weeks old)[1]
Doses: 10 mg/kg Route of Administration: 10 mg/kg; one time/day; 25 days Experimental Results: Prevented TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. |
| References |
| Molecular Formula |
C19H19N5O
|
|---|---|
| Molecular Weight |
333.39
|
| Exact Mass |
333.158
|
| Elemental Analysis |
C, 68.45; H, 5.74; N, 21.01; O, 4.80
|
| CAS # |
301326-22-7
|
| PubChem CID |
3091786
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| Appearance |
Yellow to orange solid
|
| Density |
1.2±0.1 g/cm3
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| Boiling Point |
469.4±45.0 °C at 760 mmHg
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| Flash Point |
237.7±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
3.48
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
482
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=NN1C)NC2=CC=C(/N=N/C3=CC=CC=C3C)C=C2C
|
| InChi Key |
LKTNEXPODAWWFM-GHVJWSGMSA-N
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| InChi Code |
InChI=1S/C19H19N5O/c1-13-6-4-5-7-17(13)23-22-15-8-9-16(14(2)12-15)21-19(25)18-10-11-20-24(18)3/h4-12H,1-3H3,(H,21,25)/b23-22+
|
| Chemical Name |
(E)-1-methyl-N-(2-methyl-4-(o-tolyldiazenyl)phenyl)-1H-pyrazole-5-carboxamide
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| Synonyms |
CH223191; CH-223191; CH 223191.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 66 mg/mL (198.0 mM)
Water:<1 mg/mL Ethanol: 4 mg/mL (12.0 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.33 mg/mL (0.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 20 mg/mL (59.99 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9995 mL | 14.9975 mL | 29.9949 mL | |
| 5 mM | 0.5999 mL | 2.9995 mL | 5.9990 mL | |
| 10 mM | 0.2999 mL | 1.4997 mL | 2.9995 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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