1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. CCR2 antagonist 4

CCR2 antagonist 4 (Synonyms: Teijin compound 1)

Cat. No.: HY-108323 Purity: 100.00%
Handling Instructions

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.

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

CCR2 antagonist 4 Chemical Structure

CCR2 antagonist 4 Chemical Structure

CAS No. : 226226-39-7

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5 mg USD 228 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

CCR2b

180 nM (IC50)

In Vitro

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 Vivo

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].

Molecular Weight

439.86

Formula

C₂₁H₂₁ClF₃N₃O₂

CAS No.

226226-39-7

SMILES

O=C(NCC(N[[email protected]]1CN(CC2=CC=C(Cl)C=C2)CC1)=O)C3=CC=CC(C(F)(F)F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (113.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2735 mL 11.3673 mL 22.7345 mL
5 mM 0.4547 mL 2.2735 mL 4.5469 mL
10 mM 0.2273 mL 1.1367 mL 2.2735 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: ≥ 2.5 mg/mL (5.68 mM); Clear solution

  • 2.

    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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 100.00%

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Keywords:

CCR2 antagonist 4Teijin compound 1Teijin compound1Teijin compound-1CCRCC chemokine receptorchemokineschronicinflammatoryCCR2bMCP-1chemotaxisInhibitorinhibitorinhibit

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Product name:
CCR2 antagonist 4
Cat. No.:
HY-108323
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