![CCR2-RA-[R]](/upload/0201/6381779496714458961309163800.png)
| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
CCR2-RA-[R] targets the CCR2 chemokine receptor. CCR2 is a G protein-coupled receptor that is expressed on various immune cells, including monocytes and macrophages. It binds to chemokine CCL2 (MCP-1), which is a key mediator of monocyte recruitment to sites of inflammation. By binding to CCR2, CCR2-RA-[R] antagonizes the receptor, blocking CCL2-mediated signaling and monocyte migration.
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| ln Vitro |
Many small chemical antagonists of the chemokine receptor CCR2, a G protein-coupled receptor linked to a number of disorders characterized by chronic inflammation, have been created. CCR2-RA-[R] has a pIC50 value of 6.1 and replaces [125I]CCL2 from CCR2. For CCR2 and CCR5, CCR2-RA-[R] had pKDs of 8.8±0.1 and 7.0±0.1, respectively [2]. By preventing activation-related conformational changes and the creation of the G-protein binding interface, CCR2-RA-[R] non-competitively suppresses CCR2. The binding pocket of CCR2-RA-[R] is strongly occluded and has a well-balanced hydrophobic and polar composition, both of which contribute to the pocket's "drugability" [3].
CCR2-RA-[R] is a potent and selective antagonist of the CCR2 chemokine receptor. It is the R-enantiomer of the CCR2 antagonist. It blocks CCL2-mediated signaling and monocyte migration in cellular models. Its selectivity for CCR2 over other chemokine receptors makes it a valuable research tool. |
| ln Vivo |
Specific in vivo activity data for CCR2-RA-[R] is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of CCR2 inhibition and its impact on inflammation, monocyte recruitment, and disease progression. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties.
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| Enzyme Assay |
CCR2-RA-[R]'s activity as a CCR2 antagonist is assessed using in vitro binding assays that measure its ability to inhibit the binding of CCL2 to CCR2. These assays may include radioligand binding assays or fluorescence-based competition assays. Its effects on CCR2-mediated signaling are assessed using functional assays such as calcium mobilization or chemotaxis assays.
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| Cell Assay |
Cellular assays for CCR2-RA-[R] involve treating immune cells expressing CCR2 with the compound and measuring its effects on CCL2-induced signaling and migration. Calcium mobilization assays and chemotaxis assays are commonly used. Its effects on monocyte recruitment are assessed.
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| Animal Protocol |
In vivo animal model protocols for CCR2-RA-[R] would involve its administration to animal models of inflammatory diseases. The compound's effects on monocyte infiltration, inflammation, and disease severity would be assessed.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for CCR2-RA-[R] is not extensively detailed in the available literature. As a small molecule antagonist, its pharmacokinetic properties would need to be evaluated in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of CCR2-RA-[R] has not been extensively characterized. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References |
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| Additional Infomation |
CCR2-RA-[R] (CAS# 512177-83-2) is a research compound used to study CCR2 chemokine receptor function. It is a potent and selective antagonist of CCR2. It is used in research to study inflammation, monocyte recruitment, and immune responses. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C18H19CLFNO3
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| Molecular Weight |
351.8
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| Exact Mass |
351.104
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| CAS # |
512177-83-2
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| PubChem CID |
12093170
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| Appearance |
White to off-white solid powder
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| Density |
1.383g/cm3
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| Boiling Point |
482.6ºC at 760 mmHg
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| Flash Point |
245.7ºC
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| Index of Refraction |
1.605
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| LogP |
4.24
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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 |
3
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| Heavy Atom Count |
24
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| Complexity |
559
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)C1=C(C(=O)N([C@@H]1C2CCCCC2)C3=C(C=C(C=C3)Cl)F)O
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| InChi Key |
VQNLJXWZGVRLBA-MRXNPFEDSA-N
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| InChi Code |
InChI=1S/C18H19ClFNO3/c1-10(22)15-16(11-5-3-2-4-6-11)21(18(24)17(15)23)14-8-7-12(19)9-13(14)20/h7-9,11,16,23H,2-6H2,1H3/t16-/m1/s1
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| Chemical Name |
(5R)-4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-1,5-dihydro-3-hydroxy-2H-pyrrol-2-one
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| Synonyms |
CCR2 RA [R]CCR2RA[R] CCR2-RA-[R]
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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 |
| 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 : ~37.5 mg/mL (~106.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (10.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 37.5 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: ≥ 3.75 mg/mL (10.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 37.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8425 mL | 14.2126 mL | 28.4252 mL | |
| 5 mM | 0.5685 mL | 2.8425 mL | 5.6850 mL | |
| 10 mM | 0.2843 mL | 1.4213 mL | 2.8425 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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