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1427058-33-0

1427058-33-0 structure
1427058-33-0 structure
  • Name: E 6130
  • Chemical Name: E6130
  • CAS Number: 1427058-33-0
  • Molecular Formula: C28H37ClF3N3O3
  • Molecular Weight: 556.06
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2018-09-08 17:42:26
  • Modify Date: 2025-08-20 17:42:11
  • E6130 is an orally available and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.

Name E6130
Description E6130 is an orally available and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
Related Catalog
Target

CX3CR1

In Vitro E6130 is an orally available 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].
References

[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.

Molecular Formula C28H37ClF3N3O3
Molecular Weight 556.06
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