Izuforant
Based on 1 Customer Validation
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies.
For research use only. We do not sell to patients.
- Purity: 98.88%
- CAS No.: 1429374-83-3
- Formula: C12H12BrN7
- Molecular Weight:334.17
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
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Human H4 Receptor 36 nM (IC50) |
h5-HT3R 9.1 μM (IC50) |
Izuforant (JW1601) (Compound 24) shows metabolic stability with CLh,int values of 3.05 and 1.33 mL/min/mg in mouse and human, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Izuforant (100 mg/kg; p.o.; twice a day for 3 weeks) inhibits oxazolone-induced atopic dermatitis in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female, ICR mice (8 weeks old)[1]
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Dosage:50 mg/kg
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Administration:Oral administration, once
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Result:Decreased histamine-and substance P-induced itching.
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Animal Model:Female, Balb/c mice (6 weeks old, 20±3 g)[1]
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Dosage:100 mg/kg
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Administration:Oral administration, twice a day for 3 weeks
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Result:Inhibited oxazolone-induced atopic dermatitis (51.2% inhibition).
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Animal Model:ICR mouse (20~30 g) and SD rat (200~300 g)[1]
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Dosage:50 mg/kg for mice and 10 mg/kg for rats
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Administration:Oral administration (Pharmacokinetic Analysis)
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Result:Pharmacokinetics parameter of Izuforant (Compound 24)[1]
Compound Mouse Rat t1/2 (h) Cmax (μg/mL) AUCinf (μg•hr/mL) t1/2 (h) Cmax (μg/mL) AUCinf (μg•hr/mL) Izuforant 0.96 18.87 32.17 1.30 2.42 4.51
Chemical Information
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CAS No. 1429374-83-3
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Appearance Solid
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Molecular Weight 334.17
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Formula C12H12BrN7
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Color Off-white to light green
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SMILES
CNC1CN(C2=NC3=NC=C(Br)C=C3N4C2=NN=C4)C1
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Synonyms
JW1601
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (299.25 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (14.96 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9925 mL | 14.9624 mL | 29.9249 mL | 74.8122 mL |
| 5 mM | 0.5985 mL | 2.9925 mL | 5.9850 mL | 14.9624 mL | |
| 10 mM | 0.2992 mL | 1.4962 mL | 2.9925 mL | 7.4812 mL | |
| 15 mM | 0.1995 mL | 0.9975 mL | 1.9950 mL | 4.9875 mL | |
| 20 mM | 0.1496 mL | 0.7481 mL | 1.4962 mL | 3.7406 mL | |
| 25 mM | 0.1197 mL | 0.5985 mL | 1.1970 mL | 2.9925 mL | |
| 30 mM | 0.0997 mL | 0.4987 mL | 0.9975 mL | 2.4937 mL | |
| 40 mM | 0.0748 mL | 0.3741 mL | 0.7481 mL | 1.8703 mL | |
| 50 mM | 0.0598 mL | 0.2992 mL | 0.5985 mL | 1.4962 mL | |
| 60 mM | 0.0499 mL | 0.2494 mL | 0.4987 mL | 1.2469 mL | |
| 80 mM | 0.0374 mL | 0.1870 mL | 0.3741 mL | 0.9352 mL | |
| 100 mM | 0.0299 mL | 0.1496 mL | 0.2992 mL | 0.7481 mL |
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