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Chemical Structure : E 6130
CAS No.: 1427058-33-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $398 | In stock | |
| 10 mg | $588 | In stock | |
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| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 556.067 | |
| Formula | C28H37ClF3N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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) |
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1. Wakita H, et al. Mol Pharmacol. 2017 Nov;92(5):502-509.
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