CXCR4 modulator-2

Names

[ CAS No. ]:
2488943-55-9

[ Name ]:
CXCR4 modulator-2

Biological Activity

[Description]:

CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CXCR
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Immunology/Inflammation >> CXCR

[Target]

CXCR4:1.25 nM (IC50)


[In Vivo]

CXCR4 modulator-2 (10 mg/kg; IP; single dosage) significantly reduces the edema weights (∼50%) in the lesion and decreases the expression of CXCR4s[1]. Animal Model: male nude mice (6 weeks, 20 g; subcutaneous injection of 50 μL of λ-carrageenan)[1] Dosage: 10 mg/kg Administration: IP; single dosage Result: Significantly reduced the edema weights (∼50%) in the lesion and decreased the expression of CXCR4s.

[References]

[1]. Oum YH, et al. Discovery of novel aminopiperidinyl amide CXCR4 modulators through virtual screening and rational drug design. Eur J Med Chem. 2020;201:112479.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H32N8O2

[ Molecular Weight ]:
428.53

Related Compounds