Zelnecirnon
Based on 1 Customer Validation
Zelnecirnon (RPT193) is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. Zelnecirnon can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.71%
- No. CAS: 2366152-15-8
- Fòrmula: C27H34Cl3N5O2
- Peso molecular:566.95
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
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CCR4 |
Zelnecirnon (1 nM-10 μM) inhibits Th2 cells chemotaxis or migration with IC50s of ~370 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute ovalbumin (OVA)-induced atopic dermatitis model in mouse[2]
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Dosage:100 mg/kg
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Administration:Oral gavage; once daily; for 2 days, started 1 day before OVA-challenge (in mouse ear)
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Result:Decreased the ear thickness significantly.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2366152-15-8
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Appearance Solid
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Peso molecular 566.95
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Fòrmula C27H34Cl3N5O2
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Color White to off-white
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SMILES
C[C@H](C1=C(C=C(C=C1)Cl)Cl)NC2=NC(N3CC([C@@H]4CN([C@H]5C[C@@](C)(C5)C(O)=O)CCC4)C3)=NC(C)=C2Cl
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Synonyms
RPT193
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
Methanol : 250 mg/mL (440.96 mM; Need ultrasonic)
DMSO : 100 mg/mL (176.38 mM; Need ultrasonic; 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 / Methanol | 1 mM | 1.7638 mL | 8.8191 mL | 17.6382 mL | 44.0956 mL |
| 5 mM | 0.3528 mL | 1.7638 mL | 3.5276 mL | 8.8191 mL | |
| 10 mM | 0.1764 mL | 0.8819 mL | 1.7638 mL | 4.4096 mL | |
| 15 mM | 0.1176 mL | 0.5879 mL | 1.1759 mL | 2.9397 mL | |
| 20 mM | 0.0882 mL | 0.4410 mL | 0.8819 mL | 2.2048 mL | |
| 25 mM | 0.0706 mL | 0.3528 mL | 0.7055 mL | 1.7638 mL | |
| 30 mM | 0.0588 mL | 0.2940 mL | 0.5879 mL | 1.4699 mL | |
| 40 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL | 1.1024 mL | |
| 50 mM | 0.0353 mL | 0.1764 mL | 0.3528 mL | 0.8819 mL | |
| 60 mM | 0.0294 mL | 0.1470 mL | 0.2940 mL | 0.7349 mL | |
| 80 mM | 0.0220 mL | 0.1102 mL | 0.2205 mL | 0.5512 mL | |
| 100 mM | 0.0176 mL | 0.0882 mL | 0.1764 mL | 0.4410 mL |
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