详情描述
Y-320 is an orally active potent immunomodulator. Y-320 inhibits IL-15-induced IL-17 production by CD4 T cells with an IC50 of 20 nM. Therapeutic treatment with Y-320 (0.3 to 3 mg/kg orally) significantly inhibited the progression of arthritis and joint destruction in type II collagen-induced arthritis (CIA) in DBA/1J mice. Y-320 inhibited the elevation of IL-17 mRNA expression in the joint of CIA mice. Concomitant treatment with Y-320 and anti-mouse TNF-alpha antibody showed a synergistic effect in mouse CIA. Moreover, therapeutic treatment with Y-320 (0.3 and 1 mg/kg orally) ameliorated CIA in cynomolgus monkeys.
Product information
CAS Number: 288250-47-5
Molecular Weight: 505.01
Formula: C27H29ClN6O2
Chemical Name: 1-(4-chlorophenyl)-N-(3-cyano-4-(4-morpholinopiperidin-1-yl)phenyl)-5-methyl-1H-pyrazole-4-carboxamide
Smiles: CC1=C(C=NN1C1C=CC(Cl)=CC=1)C(=O)NC1=CC(C#N)=C(C=C1)N1CCC(CC1)N1CCOCC1
InChiKey: BWZNJVZTAWBIFG-UHFFFAOYSA-N
InChi: InChI=1S/C27H29ClN6O2/c1-19-25(18-30-34(19)24-5-2-21(28)3-6-24)27(35)31-22-4-7-26(20(16-22)17-29)33-10-8-23(9-11-33)32-12-14-36-15-13-32/h2-7,16,18,23H,8-15H2,1H3,(H,31,35)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: (25°C) DMSO: 11 mg/mL(21.78 mM). Water: Insoluble.
Shipping Condition: Shipped under ambien...
Storage Condition: Dry, dark and -20 oC...
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
Y-320 was used at 0.1-1 µM final concentration in various in vitro assays.
In Vivo:
Y-320 was administered orally at 0.3-3 mg/kg once day in mouse models.
References:
- Ushio H, et al. A New Phenylpyrazoleanilide, Y-320, Inhibits Interleukin 17 Production and Ameliorates Collagen-Induced Arthritis in Mice and Cynomolgus Monkeys. (2013) Pharmaceuticals (Basel) 7(1), 1-17.
Products are for research use only. Not for human use.