1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. E6130

E6130 

Cat. No.: HY-107456 Purity: >98.0%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & 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].

Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (449.59 mM)

*"≥" means soluble, but saturation unknown.

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

E6130E 6130E-6130CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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E6130
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HY-107456
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