Ilacirnon
Based on 1 publication(s) in Google Scholar
CCX140 (CCX140-B) is a potent CCR2 antagonist.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.05%
- CAS. Nr.: 1100318-47-5
- Formel: C20H13ClF3N5O3S
- Molecular Weight:495.86
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Ilacirnon
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Biologische Aktivität
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hCCR2 2.3 nM (Kd, in monocytes) |
CCR2 3 nM (IC50, in THP-1 cells) |
CCR5 7 μM (IC50, in Activated T lymphocytes) |
CCX140 (CCX140-B) potently inhibits CCL2-induced chemotaxis of purified human blood monocytes with IC50 values of 8 nM in buffer and 200 nM in the presence of 100% human serum. CCX140 also inhibits CCL2-induced Ca2+ mobilization in monocytes with an IC50 value of 3 nM. CCX140 inhibits the binding of 125I-CCL2 to monocytes with an IC50 value of 17 nM. CCX140 has a Kd value of 2.3 nM toward hCCR2. CCX140 also inhibits monocyte chemotaxis mediated by the other CCR2 ligands: CCL8/MCP-2, CCL7/MCP-3, and CCL13/MCP-4[1].
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.
Chemical Information
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CAS. Nr. 1100318-47-5
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Appearance Solid
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Molecular Weight 495.86
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Formel C20H13ClF3N5O3S
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Color Light yellow to yellow
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SMILES
FC(F)(F)C1=CC(S(=O)(NC2=CC(C)=CN=C2C(C3=NC=NC4=C3C=CN4)=O)=O)=CC=C1Cl
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Synonyms
CCX140; CCX140-B
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
CCL2 promotes macrophages-associated chemoresistance via MCPIP1 dual catalytic activities in multiple myeloma. [Abstract]2019 Oct 14;10(10):781. PMID: 31611552
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (201.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.25 mg/mL (0.50 mM; Need ultrasonic and warming)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.04 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.
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.
Protokoll
Mice: CCX140 is formulated as a solution in 1% hydroxypropyl methylcellulose. Male uninephrectomized hCCR2 KI mice are rendered diabetic with the high-fat diet and dosed with 100 mg/kg CCX140, but for 8 wk of dosing. Eight-week-old male hCCR2 KI Lepr db/db mice are similarly dosed with 100 mg/kg CCX140 for 6 wk[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Sullivan T, et al. CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice. Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97. [Content Brief]
[2]. Sullivan TJ, et al. Experimental evidence for the use of CCR2 antagonists in the treatment of type 2 diabetes. Metabolism. 2013 Nov;62(11):1623-32. [Content Brief]
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 | 2.0167 mL | 10.0835 mL | 20.1670 mL | 50.4175 mL |
| 5 mM | 0.4033 mL | 2.0167 mL | 4.0334 mL | 10.0835 mL | |
| 10 mM | 0.2017 mL | 1.0083 mL | 2.0167 mL | 5.0417 mL | |
| 15 mM | 0.1344 mL | 0.6722 mL | 1.3445 mL | 3.3612 mL | |
| 20 mM | 0.1008 mL | 0.5042 mL | 1.0083 mL | 2.5209 mL | |
| 25 mM | 0.0807 mL | 0.4033 mL | 0.8067 mL | 2.0167 mL | |
| 30 mM | 0.0672 mL | 0.3361 mL | 0.6722 mL | 1.6806 mL | |
| 40 mM | 0.0504 mL | 0.2521 mL | 0.5042 mL | 1.2604 mL | |
| 50 mM | 0.0403 mL | 0.2017 mL | 0.4033 mL | 1.0083 mL | |
| 60 mM | 0.0336 mL | 0.1681 mL | 0.3361 mL | 0.8403 mL | |
| 80 mM | 0.0252 mL | 0.1260 mL | 0.2521 mL | 0.6302 mL | |
| 100 mM | 0.0202 mL | 0.1008 mL | 0.2017 mL | 0.5042 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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