| Cas No.: | 1427058-33-0 |
| Chemical Name: | [(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) |
| Synonyms: | E-6130;E6130 |
| Formula: | C28H37ClF3N3O3 |
| M.Wt: | 556.067 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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 TumorsPhase 1 Clinical |

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