E 6130

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服的 CX3C 趋化因子受体 1 (CX3CR1) 调节剂，可抑制 fractalkine 诱导的人外周血 NK 细胞的趋化性，IC50 为 4.9 nM。

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; shows no significant agonistic or antagonistic activity (EC50 and IC50>10 uM) for any other chemokine receptors; 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; inhibits the migration of CX3CR1+ immune cells, and ameliorates several inflammatory bowel disease-related parameters in murine CD4+CD45RBhigh T-cell-transfer colitis model.Solid Tumors Phase 1 Clinical.

E6130 is an orally active 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.

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.

E-6130 | E6130

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Cancer

Solid Tumors

1427058-33-0

556.067

C28H37ClF3N3O3

>98% (HPLC)

DMSO : ≥ 250 mg/mL 449.59 mM

CC1CN(CC1(CC(=O)O)C(=O)NC2CCN(CC2)CC3=CCCCC3)CC4=C(C=CC=C4Cl)C(F)(F)F

[(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)

(-20℃)

With Ice Pack

≥ 2 years