2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. CXCR4-IN-3

CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research.

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CXCR4-IN-3 Chemical Structure

CXCR4-IN-3 Chemical Structure

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CXCR4-IN-3 Related Antibodies

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Description

CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research[1].

IC50 & Target

CXCR4

3.2 nM (IC50)

In Vivo

CXCR4-IN-3 (compound XVI) (25 mg/kg, IG, twice a day for 14 consecutive days) alleviates DSS (dextran sulfate sodium)-induced IBD (inflammatory bowel disease) and is associated with reduced numbers of inflammatory cells and reduced secretion of inflammatory factors[1].
CXCR4-IN-3 (iv (2 mg/kg) ig (20 mg/kg); once) shows reasonable pharmacokinetic properties[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (8 weeks, n=8 per group, DSS-Induced Colitis Model)[1]
Dosage: 25 mg/kg
Administration: Intragastrically, 100 μL/10 g, twice a day for 14 consecutive days
Result: Markedly relieved the condition of IBD; Significantly decreased the myeloperoxidase (MPO) levels; Blocked chronic inflammation of the intestinal tract.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: iv (2 mg/kg) ig (20 mg/kg)
Administration: IV or IG, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of CXCR4-IN-3 in male Sprague-Dawley rats[1].
IV (2 mg/kg) IG (20 mg/kg)
Tmax (h) 0.08 0.25
t1/2 (h) 0.81±0.10 1.71±0.08
Cmax (ng/mL) 351.42±18.92 1436.41±805.36
AUC0-t (ng/mL∗h) 330.37±22.00 3010.81±283.96
AUC0-∞ (ng/mL∗h) 340.29±26.61 3070.77±325.73
CL (mL/h/kg) 5901.52±463.48 6565.45±741.43
V (mL/kg) 6037.79±278.59 16161.66±1798.44
F (%) 91.14
Molecular Weight

339.43

Formula

C20H25N3O2
SMILES

O=C(C1=CC=CO1)N2CCN(C3CCN(C4=CC=CC=C4)CC3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CXCR4-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CXCR4-IN-3CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsinflammatory bowel diseaseantichemotacticorally activeInhibitorinhibitorinhibit

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