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E6130 may be effective in the treatment of inflammatory bowel disease and is a highly selective CX3CR1 regulator for oral administration.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $3,128 | 8-10 weeks | |
25 mg | $4,389 | 8-10 weeks | |
50 mg | $6,578 | 8-10 weeks | |
100 mg | $9,859 | 8-10 weeks |
Description | E6130 may be effective in the treatment of inflammatory bowel disease and is a highly selective CX3CR1 regulator for oral administration. |
In vitro | 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.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. |
In vivo | E6130(10 or 30mg /kg, p.o.) reduced some parameters associated with inflammatory bowel disease in a mouse model of CD4+ CD45RBhigh t cell metastatic colitis and a mouse model of oxazolidin-induced colitis. |
Molecular Weight | 556.06 |
Formula | C28H37ClF3N3O3 |
Cas No. | 1427058-33-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (449.59 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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