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CCR2-RA-[R]
CAS No. 512177-83-2
CCR2-RA-[R]( CCR2-RA [R] )
Catalog No. M14769 CAS No. 512177-83-2
A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 67 | In Stock |
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| 2MG | 37 | In Stock |
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| 5MG | 61 | In Stock |
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| 10MG | 92 | In Stock |
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| 25MG | 187 | In Stock |
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| 50MG | 298 | In Stock |
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| 100MG | 410 | In Stock |
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| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameCCR2-RA-[R]
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.
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DescriptionA potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.
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In VitroThe chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”.
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In Vivo——
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SynonymsCCR2-RA [R]
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PathwayGPCR/G Protein
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TargetChemokine Receptor
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RecptorChemokine Receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number512177-83-2
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Formula Weight351.802
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Molecular FormulaC18H19ClFNO3
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 125 mg/mL 355.32 mM; H2O : < 0.1 mg/mL
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SMILESO=C1N(C2=CC=C(Cl)C=C2F)[C@H](C3CCCCC3)C(C(C)=O)=C1O
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Chemical Name(R)-4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Zheng Y, et al. Nature. 2016 Dec 15;540(7633):458-461.
2. Zweemer AJ, et al. Mol Pharmacol. 2013 Oct;84(4):551-61.
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