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CCR2-RA-[R]

Catalog No. T14900Cas No. 512177-83-2

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

CCR2-RA-[R]

CCR2-RA-[R]

Purity: 99.70%
Catalog No. T14900Cas No. 512177-83-2
CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).
Pack SizePriceAvailabilityQuantity
2 mg$39In Stock
5 mg$64In Stock
10 mg$97In Stock
25 mg$197In Stock
50 mg$320In Stock
100 mg$441In Stock
1 mL x 10 mM (in DMSO)$70In Stock
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Purity:99.70%
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Product Introduction

Bioactivity
Description
CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).
Targets&IC50
CCR2:103 nM (in U2OS-CCR2 cells)
In vitro
CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. 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[2]. The 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. 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”[3].
Chemical Properties
Molecular Weight351.8
FormulaC18H19ClFNO3
Cas No.512177-83-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 0.1 mg/mL (insoluble)
DMSO: 125 mg/mL (355.32 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8425 mL14.2126 mL28.4252 mL142.1262 mL
5 mM0.5685 mL2.8425 mL5.6850 mL28.4252 mL
10 mM0.2843 mL1.4213 mL2.8425 mL14.2126 mL
20 mM0.1421 mL0.7106 mL1.4213 mL7.1063 mL
50 mM0.0569 mL0.2843 mL0.5685 mL2.8425 mL
100 mM0.0284 mL0.1421 mL0.2843 mL1.4213 mL

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