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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-E 6130
E 6130

Chemical Structure : E 6130

CAS No.: 1427058-33-0

E 6130 (E-6130;E6130)

货号: PC-60779Not For Human Use, Lab Use Only.

E6130 is a potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

E6130 is a potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.
E6130 shows no significant agonistic or antagonistic activity (EC50 and IC50>10 uM) for any other chemokine receptors.
E6130  induces the down-regulation of CX3CR1 on the cell surface of CD56+ NK cells with IC50 of 5.2 nM, shows agonistic activity with respect to [35S]GTPγS binding (EC50=133 nM) and β-arrestin recruitment (EC50=2.4 uM) in CX3CR1-expressing CHO-K1 membrane.
E6130 inhibits the migration of CX3CR1+ immune cells, and ameliorates several inflammatory bowel disease-related parameters in murine CD4+CD45RBhigh T-cell-transfer colitis model.

物理化学性质&存储条件

分子量 556.067
分子式 C28H37ClF3N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[(3S,4R)-1-[2-Chloro-6-(trifluoromethyl)benzyl]-3-{[1-(cyclohex-1-en-1-ylmethyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid (2S)-hydroxy(phenyl)

参考文献

1. Wakita H, et al. Mol Pharmacol. 2017 Nov;92(5):502-509.

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