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E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease. In Vitro E6130 is an orally active and highly selective CX3CR1 modulator, inhibits the fractalkine-induced chemotaxis of human peripheral blood natural killer cells (IC 50 , 4.9 nM), and down-regulates CX3CR1 on the cell surface of CD56 + NK cells with an EC 50 value of 5.2 nM. E6130 also shows agonistic activity via CX3CR1 with respect to GTPγS binding (EC 50 = 133 nM) and β-arrestin recruitment (EC 50 = 2.4 μM) in CX3CR1-expressing CHO-K1 membrane but show no antagonistic activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo E6130 (10 or 30 mg/kg, p.o.) reduces several inflammatory bowel disease-related parameters in a murine CD4 + CD45RB high T-cell-transfer colitis model and a murine oxazolone-induced colitis model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CX3CR1
中文名称
E6130
英文名称
E6130
中文别名
-
英文别名
1427058-33-0 | CHC05833 | HY-107456 | SCHEMBL14760920 | E6130 | 2-[(3S,4R)-1-{[2-Chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl) piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid | (3S,4R)-1-[[2-Chloro-6-(trifluoromet
CAS号
1427058-33-0
分子式
C28H37ClF3N3O3
分子量
556.06 g/mol
精确质量
≥98%
PSA
72.900 Ų
Logp
2.300
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E6130 1ml

品牌:阿拉丁
货号:E656709-1ml
级别: 10mM in DMSO
货期:30天
已售 214 件
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