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[CAS NO. 1427058-33-0] E6130
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-107456 |
| Brand: | MCE |
| CAS: | 1427058-33-0 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 556.06 |
| Molecular Formula | C28H37ClF3N3O3 |
| SMILES | C[C@@H](C1)[C@@](C(NC2CCN(CC3=CCCCC3)CC2)=O)(CC(O)=O)CN1CC4=C(C(F)(F)F)C=CC=C4Cl |
1 Publications Citing Use of MCE
Summary
E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
IC50 & Target
CX3CR1 [1]
In Vitro
E6130 is an orally active and highly selective CX3CR1 modulator, inhibits the fractalkine-induced chemotaxis of human peripheral blood natural killer cells (IC 50 , 4.9 nM), and down-regulates CX3CR1 on the cell surface of CD56 + NK cells with an EC 50 value of 5.2 nM. E6130 also shows agonistic activity via CX3CR1 with respect to GTPγS binding (EC 50 = 133 nM) and β-arrestin recruitment (EC 50 = 2.4 μM) in CX3CR1-expressing CHO-K1 membrane but show no antagonistic activity [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
E6130 (10 or 30 mg/kg, p.o.) reduces several inflammatory bowel disease-related parameters in a murine CD4 + CD45RB high T-cell-transfer colitis model and a murine oxazolone-induced colitis model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02902978 | EA Pharma Co., Ltd.|Eisai Inc. |
Japanese Healthy Adult Male Participants
|
September 26, 2016 | Phase 1 |
| NCT03390647 | EA Pharma Co., Ltd.|Eisai Inc. |
Healthy Participants
|
December 21, 2017 | Phase 1 |
Appearance
Solid
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
DMSO : ≥ 250 mg/mL ( 449.59 mM )
* "≥" means soluble, but saturation unknown.
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 |
Synonyms
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