product name WZ811
Description: WZ811 is a highly potent, selective, competitive CXCR4 antagonist. It shows subnanomolar potency (EC50 = 0.3 nM) in an affinity binding assay. WZ811 efficiently inhibits CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cyclic adenosine monophophate (cAMP) levels (EC50 = 1.2 nM) and SDF-1 induced Matrigel invasion (EC50 = 5.2 nM).
References: J Med Chem. 2007 Nov 15;50(23):5655-64.
290.36
Formula
C18H18N4
CAS No.
55778-02-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 30 mg/mL (103.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409525
| In Vitro |
In vitro activity: WZ811 is a highly potent competitive antagonist of CXCR4. WZ811 is effective in counteracting SDF-1 on cAMP reduction at doses as low as a few nanomoles. WZ811 blocks SDF-1-mediated invasion with EC50 of 5.2 NM. Kinase Assay: Cell Assay: In the cAMP assay, WZ811 reduces the effect on cAMP caused by 150ng/ml SDF-1 significantly. It also blocks the SDF-1 induced Matrigel invasion with EC50 value of 5.2nM. Since CXCR4 is involved in the pathogeneses of a wide range of infectious, inflammatory and other diseases, WZ811 is developed for the treatment of various CXCR4-related diseases. It is reported to have weak anti-HIV activity in cell culture. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2007 Nov 15;50(23):5655-64. |
