CCR2 antagonist 4
Based on 6 publication(s) in Google Scholar
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
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- Pureza: 100.0%
- No. CAS: 226226-39-7
- Fòrmula: C21H21ClF3N3O2
- Peso molecular:439.86
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) CCR2 antagonist 4
More
Actividad biológica
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CCR2b 180 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.98 μM
Compound: 1a
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Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
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[PMID: 20223662] |
| HEK293-EBNA | IC50 |
3.2 μM
Compound: 1a
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Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
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[PMID: 20223662] |
| THP-1 | EC50 |
0.02 μM
Compound: 11i(R)
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Inhibition of MCP-1 induced chemotaxis in THP-1 cells
Inhibition of MCP-1 induced chemotaxis in THP-1 cells
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[PMID: 15454236] |
| THP-1 | IC50 |
>0.3 μM
Compound: 1a
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Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
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[PMID: 20223662] |
| THP-1 | IC50 |
180 nM
Compound: 1
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Displacement of [125I]MCP1 from human CCR2b in THP1 cells
Displacement of [125I]MCP1 from human CCR2b in THP1 cells
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[PMID: 18313297] |
| THP-1 | IC50 |
24 nM
Compound: 1
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Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
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[PMID: 18313297] |
Ile263 and Thr292 in CCR2 contribute significantly to binding of Teijin compound 1 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated CCR2 antagonist 4, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4[2].
In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 226226-39-7
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Appearance Solid
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Peso molecular 439.86
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Fòrmula C21H21ClF3N3O2
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Color White to off-white
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SMILES
O=C(NCC(N[C@H]1CN(CC2=CC=C(Cl)C=C2)CC1)=O)C3=CC=CC(C(F)(F)F)=C3
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Synonyms
Teijin compound 1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Immunity
Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452 -
Nat Immunol
The lactate receptor HCAR1 drives the recruitment of immunosuppressive PMN-MDSCs in colorectal cancer. [Abstract]2025 Mar;26(3):391-403. PMID: 39905201 -
Stem Cell Res Ther
Intramyocardial injected human umbilical cord-derived mesenchymal stem cells (HucMSCs) contribute to the recovery of cardiac function and the migration of CD4+ T cells into the infarcted heart via CCL5/CCR5 signaling. [Abstract]2022 Jun 11;13(1):247. PMID: 35690805 -
Mediators Inflamm
Convergent Multistage Evidence Implicates the CCR2-Artemin Immune-Inflammation Axis in Acute Myeloid Leukemia. [Abstract]2026 Jan 31:2026:2476470. PMID: 41624379 -
FASEB J
CCR2 inhibitor strengthens the adiponectin effects against myocardial injury after infarction. [Abstract]2023 Aug;37(8):e23039. PMID: 37392374 -
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (113.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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.
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 (5.68 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 (5.68 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 (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Moree WJ, et al. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1869-73. [Content Brief]
[2]. Hall SE, et al. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol. 2009 Jun;75(6):1325-36. [Content Brief]
[3]. Calin M, et al. VCAM-1 directed target-sensitive liposomes carrying CCR2 antagonists bind to activated endothelium and reduce adhesion and transmigration of monocytes. Eur J Pharm Biopharm. 2015 Jan;89:18-29. [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 | 2.2735 mL | 11.3673 mL | 22.7345 mL | 56.8363 mL |
| 5 mM | 0.4547 mL | 2.2735 mL | 4.5469 mL | 11.3673 mL | |
| 10 mM | 0.2273 mL | 1.1367 mL | 2.2735 mL | 5.6836 mL | |
| 15 mM | 0.1516 mL | 0.7578 mL | 1.5156 mL | 3.7891 mL | |
| 20 mM | 0.1137 mL | 0.5684 mL | 1.1367 mL | 2.8418 mL | |
| 25 mM | 0.0909 mL | 0.4547 mL | 0.9094 mL | 2.2735 mL | |
| 30 mM | 0.0758 mL | 0.3789 mL | 0.7578 mL | 1.8945 mL | |
| 40 mM | 0.0568 mL | 0.2842 mL | 0.5684 mL | 1.4209 mL | |
| 50 mM | 0.0455 mL | 0.2273 mL | 0.4547 mL | 1.1367 mL | |
| 60 mM | 0.0379 mL | 0.1895 mL | 0.3789 mL | 0.9473 mL | |
| 80 mM | 0.0284 mL | 0.1421 mL | 0.2842 mL | 0.7105 mL | |
| 100 mM | 0.0227 mL | 0.1137 mL | 0.2273 mL | 0.5684 mL |
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