| Bioactivity | CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM)[1]. |
| Invitro | CXCR4 antagonist 4 (Compound 30, 0.1~10 µM, 48 hours) displays the inhibition potencies against the X4 virus in TZM-bl cells (IC50=7 nM) [1]. Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | CXCR4 antagonist 4 (3, 10, 30 mg/kg) demonstrates better oral Bioavailability in a dose dependent and reached 27% for the 30 mg/kg[1].Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice[1] Route |
| Name | CXCR4 antagonist 4 |
| Formula | C29H41F2N5 |
| Molar Mass | 497.67 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Jecs E, et al. Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles. J Med Chem. 2022, 65(5):4058-4084. |
CXCR4 antagonist 4
CAS: F: C29H41F2N5 W: 497.67
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved P
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