E6130是一种可口服的，高度选择性的CX3CR1调节剂，有治疗炎症性肠病的潜力。
货号:ajcx12638
CAS:1427058-33-0
分子式:C28H37ClF3N3O3
分子量：556.06
溶解度:DMSO: ≥ 250 mg/mL (449.59 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.