Y320

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Y-320是一种新型苯基吡唑苯胺免疫调节剂；抑制 IL-15 刺激的 CD4 T 细胞产生 IL-17，IC50 值为 20 至 60 nM。

Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.

Y-320 (0-100 nM; 48 h) inhibits IL-17 production by murine and human CD4 T Cells stimulated with IL-15 with IC50 values of 25.7, 52.4 and 57.4 nM for murine CD4 T cells, murine Th17 cells and human CD4 T cells, respectively.Y-320 (0-100 nM; 48 h) inhibits phosphorylation of JAK1/JAK3 in murine CD4 T cells stimulated with IL-15/CXCL12/anti-CD3 mAb.Y-320 (0.25-2 μM; 48 h) enhances PTC readthrough by G418 in different cell lines.Y-320 (0-2 μM; 48 h; HDQ-P1 cells) increases cellular protein levels and ribosome biogenesis in a concentration-dependent manner.Y-320 (0-2 μM; 48 h; Tsc2-/- cells) causes a small decrease in phospho-S6K combination with G418 (100 μM).Y-320 (1 μM; 48 h; HDQ-P1 cells) up-regulates CXC chemokine expression including CXCL10, CXCL8, and CXCL2.Y-320 (500 nM; 72 h) reverses the resistance to paclitaxel in MDR cancer cells. Y-320 has the reversal index (RI) combined with Paclitaxel (0-1000 nM) are 5.5 (Bads-200), 9.4 (Bats-72) and 1.7 (Huh7-TS-48).Y-320 (500 nM; 72 h; Bads-200 cells) enhances Paclitaxel-induced G2/M arrest and enhances Paclitaxel-induced (500 nM) tumor cell apoptosis.Y-320 (0-20 μM; 72 h; Bads-200 cells) is a substrate of P-gp reverses MDR by inhibiting P-gp function. Cell Cycle Analysis Cell Line:Bads-200 cells Concentration:500 nMIncubation Time:72 hoursResult:Increased the percentage of cells at G2/M phase, from 6.3% to 42.5%.Apoptosis AnalysisCell Line:Bads-200 cells Concentration:500 nM Incubation Time:72 hours Result:Increased the ratio of apoptotic Bads-200 cells (30.8% versus 2.2%).

Y-320 (0-3 mg/kg; p.o.; daily, for 42 d) ameliorates collagen-induced arthritis (CIA) in DBA/1J mice with a reduction of IL-17 mRNA in arthritic joints.Y-320 (5 mg/kg; i.v.; every three days, for 18 d; Homozygous nude athymic mice with Bats-72 xenograft) sensitizes MDR xenograft tumor to Paclitaxel in vivo. Animal Model:Type II collagen-induced arthritis (CIA) in DBA/1J mice Dosage:0, 0.1, 0.3, 1, and 3 mg/kg Administration:Oral administration; daily, for 42 days Result:Inhibited the development of CIA and the increase in paw thickness in a dose-dependent manner.Inhibited joint destructions in a dose-dependent manner.Improved inflammation and damage in the arthritic ankle joints in CIA mice.Animal Model:Homozygous nude athymic mice with Bats-72 xenograft (female, 4-5 weeks old) Dosage:5 mg/kg; Paclitaxel (5 mg/kg)Administration:Intravenous injection; every three days, for 18 days Result:Inhibited tumor growth in Bats-72 xenografts without severe adverse effects.

Y-320 | Y320 | Y 320

Metabolic Enzyme/Protease

Lipase

ATGL

Inflammation/Immunology

——

288250-47-5

505.01

C27H29ClN6O2

>98% (HPLC)

DMSO: 11 mg/mL (21.78 mM)

O=C(C1=C(C)N(C2=CC=C(Cl)C=C2)N=C1)NC3=CC=C(N4CCC(N5CCOCC5)CC4)C(C#N)=C3

1-(4-chlorophenyl)-N-(3-cyano-4-(4-morpholinopiperidin-1-yl)phenyl)-5-methyl-1H-pyrazole-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years