1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

E6130 

Cat. No.: HY-107456
Handling Instructions

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

For research use only. We do not sell to patients.

E6130 Chemical Structure

E6130 Chemical Structure

CAS No. : 1427058-33-0

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7984 mL 8.9918 mL 17.9837 mL
5 mM 0.3597 mL 1.7984 mL 3.5967 mL
10 mM 0.1798 mL 0.8992 mL 1.7984 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

556.06

Formula

C₂₈H₃₇ClF₃N₃O₃

CAS No.

1427058-33-0

SMILES

C[[email protected]@H](C1)[[email protected]@](C(NC2CCN(CC3=CCCCC3)CC2)=O)(CC(O)=O)CN1CC4=C(C(F)(F)F)C=CC=C4Cl

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
E6130
Cat. No.:
HY-107456
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E6130

Cat. No.: HY-107456