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E6130
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
E6130图片
规格:98%
分子量:556.06
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
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.