1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR

CCR2-RA-[R] 

Cat. No.: HY-50081 Purity: 99.36% ee.: 99.55%
Handling Instructions

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.

For research use only. We do not sell to patients.

CCR2-RA-[R] Chemical Structure

CCR2-RA-[R] Chemical Structure

CAS No. : 512177-83-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 390 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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View All CCR Isoform Specific Products:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.

IC50 & Target[1]

CCR2

103 nM (IC50, in U2OS-CCR2 cells)

In Vitro

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. 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]. 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”[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (355.32 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (17.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (17.77 mM); Clear solution

References
Molecular Weight

351.80

Formula

C₁₈H₁₉ClFNO₃

CAS No.

512177-83-2

SMILES

O=C1C(O)=C(C(C)=O)[[email protected]@H](C2CCCCC2)N1C(C(F)=C3)=CC=C3Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.36% ee.: 99.55%

  • Molarity Calculator

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The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
CCR2-RA-[R]
Cat. No.:
HY-50081
Quantity:

CCR2-RA-[R]

Cat. No.: HY-50081