| Bioactivity | E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease. | ||||||||||||
| Target | CX3CR1 | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| In Vivo | 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[1]. | ||||||||||||
| Name | E6130 | ||||||||||||
| CAS | 1427058-33-0 | ||||||||||||
| Formula | C28H37ClF3N3O3 | ||||||||||||
| Molar Mass | 556.06 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Wakita H, et al. E6130, a Novel CX3C Chemokine Receptor 1 (CX3CR1) Modulator, Attenuates Mucosal Inflammation and Reduces CX3CR1+ Leukocyte Trafficking in Mice with Colitis. Mol Pharmacol. 2017 Nov;92(5):502-509. |
E6130
CAS: 1427058-33-0 F: C28H37ClF3N3O3 W: 556.06
E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bow
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