CCR2 antagonist 4 (hydrochloride)

CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM[1].

Product Specifications

CAS Number

[1313730-14-1]

Product Name Alternative

Teijin compound 1 (hydrochloride)

UNSPSC

12352005

Target

CCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ccr2-antagonist-4-hydrochloride.html

Purity

99.91

Solubility

DMSO : 250 mg/mL (ultrasonic) |Methanol : 125 mg/mL (ultrasonic)

Smiles

O=C(NCC(N[C@H]1CN(CC2=CC=C(Cl)C=C2)CC1)=O)C3=CC=CC(C(F)(F)F)=C3.[H]Cl

Molecular Formula

C21H22Cl2F3N3O2

Molecular Weight

476.32

References & Citations

[1]Moree WJ, et al. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R) -3-aminopyrrolidine series. Bioorg Med Chem Lett. 2008 Mar 15;18 (6) :1869-73.|[2]Hall SE, et al. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol. 2009 Jun;75 (6) :1325-36.|[3]Calin M, et al. VCAM-1 directed target-sensitive liposomes carrying CCR2 antagonists bind to activated endothelium and reduce adhesion and transmigration of monocytes. Eur J Pharm Biopharm. 2015 Jan;89:18-29.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

CCR2

Citation 01

Immunity. 2025 Aug 12:S1074-7613 (25) 00314-0.|University of Wisconsin. 2025.|FASEB J. 2023 Aug;37 (8) :e23039.|Nat Immunol. 2025 Mar;26 (3) :391-403.|Stem Cell Res Ther. 2022 Jun 11;13 (1) :247.