product name Y-320
Description: Y-320 is a novel, potent and orally active, phenylpyrazoleanilide immunomodulator, it inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 of 20 to 60 NM. In type II collagen-induced arthritis (CIA) mice, oral administration of Y-320 (0.3-3 mg/kg) reduced IL-17 mRNA expression and significantly inhibited the development of joint destruction and arthritis. The combination of Y-320 with anti-murine tumor necrosis factor-α (TNF-α) monoclonal antibody exhibited a synergistic effect. In cynomolgus monkeys, Y-320 (0.3-1 mg/kg) relieved CIA. These results suggested that Y-320 could be a useful candidate for therapy of rheumatoid arthritis (RA).
References: Pharmaceuticals (Basel). 2013 Dec 23;7(1):1-17.
505.01
Formula
C27H29ClN6O2
CAS No.
288250-47-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 11 mg/mL (21.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Y-320 also inhibits the production of IFN-γ and TNF-α by mouse CD4 T cells stimulated with IL-15, CXCL12, and anti-CD3 mAb. Kinase Assay: Cell Assay: Y-320 inhibited IL-17 production by CD4 T cells induced by IL-15 with IC50 values of 20-60 NM. |
|---|---|
| In Vivo | Y-320 (0.3-3 mg/kg p.o.) ameliorates collagen-induced arthritis (CIA) in Mice with a reduction of IL-17 mRNA in arthritic joints, and also shows therapeutic effects on CIA in cynomolgus monkeys. Moreover, Y-320 shows a synergistic effect in combination with anti-TNF-α mAb on chronic-progressing CIA in mice. |
| Animal model | DBA/1J mice with type II collagen-induced arthritis (CIA) |
| Formulation & Dosage | Suspended in a 0.5% hydroxypropylmethylcellulose (HPMC); 3 mg/kg; p.o. |
| References | Pharmaceuticals (Basel). 2013 Dec 23;7(1):1-17. |
