[CAS NO. 1427058-33-0] E6130

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PRODUCTS SPECIFICATIONS [1427058-33-0]

Catalog

HY-107456

Brand

MCE

CAS

1427058-33-0

DESCRIPTION [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

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

1 Publications Citing Use of MCE

[1]Cancers (Basel). 2022, 14(1), 64.

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

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 available by MCE.

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.

Synonyms

3-Pyrrolidineacetic acid, 1-[[2-chloro-6-(trifluoromethyl)phenyl]methyl]-3-[[[1-(1-cyclohexen-1-ylmethyl)-4-piperidinyl]amino]carbonyl]-4-methyl-, (3S,4R)-

(3S,4R)-1-[[2-Chloro-6-(trifluoromethyl)phenyl]methyl]-3-[[[1-(1-cyclohexen-1-ylmethyl)-4-piperidinyl]amino]carbonyl]-4-methyl-3-pyrrolidineacetic acid