E6130 |
| Catalog No.GC31763 |
E6130 est un modulateur CX3CR1 actif par voie orale et hautement sélectif, qui peut être efficace pour le traitement des maladies inflammatoires de l'intestin.
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Cas No.: 1427058-33-0
Sample solution is provided at 25 µL, 10mM.
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E6130 is an orally available and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
E6130 is an orally available and highly selective CX3CR1 modulator, inhibits the fractalkine-induced chemotaxis of human peripheral blood natural killer cells (IC50, 4.9 nM), and down-regulates CX3CR1 on the cell surface of CD56+ NK cells with an EC50 value of 5.2 nM. E6130 also shows agonistic activity via CX3CR1 with respect to GTPγS binding (EC50 = 133 nM) and β-arrestin recruitment (EC50 = 2.4 μM) in CX3CR1-expressing CHO-K1 membrane but show no antagonistic activity[1].
E6130 (10 or 30 mg/kg, p.o.) reduces several inflammatory bowel disease-related parameters in a murine CD4+ CD45RBhigh T-cell-transfer colitis model and a murine oxazolone-induced colitis model[1].
[1]. Wakita H, et al. E6130, a Novel CX3C Chemokine Receptor 1 (CX3CR1) Modulator, Attenuates Mucosal Inflammation and Reduces CX3CR1+ Leukocyte Trafficking in Mice with Colitis. Mol Pharmacol. 2017 Nov;92(5):502-509.
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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