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SRN 927

Target nature : CXCL12
CAS n° : not yet attributed?
Mecanism of action : neutralizes CXCL12 like Chalcone 4
Physico-chemical properties : solubility in buffer= 30 µM
Probe availability : request to Laboratoire d'innovation thérapeutique (UMR 7200 CNRS-unistra)
Princeps reference : Regenass, P., Abboud, D., Daubeuf, F., Riché, S., Marsol, C., Rohmer, F., Hachet-Haas, M., Hibert, M., Frossard, N., Galzi, JL., Bonnet, D. (2018). Structure-Activity Relationship Study toward the Discovery of Novel CXCL12 Neutraligands with in vivo Activity in an Allergic Eosinophilic Airway Inflammation Model. J. Med. Chem. 61(17):7671-7686. doi: 10.1021/acs.jmedchem.8b00657
More bibliography : Bonnet, D., Frossard, N., Galzi, JL., Guignabert, C., Hibert, M., Simonin, F. Muller, S. (2106) Pyrimidinone derivatives and uses thereof to neutralize the biological activity of chemokines13 July 2016. European patent application EP16305908.2
Other available information on the probe : fully inhibits binding of CXCL12 to CXCR4
Other information on the target : x
Selectivity profile : effect on CCL17, CCL22, CCL5, CCL2. other chemokines were not tested. No alert in the safety 44 assay
In vivo data : - orally bioavailable - inhibits eosinophil recruitment in the OVA mouse model of asthma - inhibits hyperalgesia linked to opiates, inflammatory, and neuropathic pain
In vitro data : KD for CXCL12 = 267 +/- 71 nM
Toxicity : no toxicity after 8 d treatment with 350 µmol/kg
Chaine SMILES : COc3cc(c2cc(c1ccc(Cl)cc1)[nH]c(=O)n2)ccc3O
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