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Y-320
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Y-320图片
CAS NO:288250-47-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
Y-320 是一种口服有效的苯吡唑苯胺免疫调节剂。Y-320 抑制 IL-15 刺激的 CD4 T 细胞产生 IL-17, 其IC50值为 20-60 nM。Y-320 增强 G418 对 TP53、DMD和COL17A1 PTC 的读入,增加细胞蛋白质水平和蛋白质合成。Y-320 与低剂量 Paclitaxel (HY-B0015) 通过诱导 G2/M 期阻滞和细胞凋亡 (apoptosis) 显著致敏多药耐药性 (MDR) 肿瘤。Y-320 可用于类风湿关节炎 (RA) 和肿瘤的研究。
生物活性

Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibitsIL-17production byCD4T cells stimulated withIL-15withIC50values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose ofPaclitaxel(HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest andapoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) andcancer[1][2][2].

IC50& Target[1]

IL-15

 

IL-17

 

体外研究
(In Vitro)

Y-320 (0-100 nM; 48 h) inhibits IL-17 production by murine and human CD4 T Cells stimulated with IL-15 with IC50values of 25.7, 52.4 and 57.4 nM for murine CD4 T cells, murine Th17 cells and human CD4 T cells, respectively[1].
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[1].
Y-320 (0.25-2 μM; 48 h) enhances PTC readthrough by G418 in different cell lines[2].
Y-320 (0-2 μM; 48 h; HDQ-P1 cells) increases cellular protein levels and ribosome biogenesis in a concentration-dependent manner[2].
Y-320 (0-2 μM; 48 h; Tsc2-/-cells) causes a small decrease in phospho-S6K combination with G418 (100 μM)[2].
Y-320 (1 μM; 48 h; HDQ-P1 cells) up-regulates CXC chemokine expression including CXCL10, CXCL8, and CXCL2[2].
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)[3].
Y-320 (500 nM; 72 h; Bads-200 cells) enhances Paclitaxel-induced G2/M arrest and enhances Paclitaxel-induced (500 nM) tumor cell apoptosis[3].
Y-320 (0-20 μM; 72 h; Bads-200 cells) is a substrate of P-gp reverses MDR by inhibiting P-gp function[3].

Cell Cycle Analysis[3]

Cell Line:Bads-200 cells
Concentration:500 nM
Incubation Time:72 hours
Result:Increased the percentage of cells at G2/M phase, from 6.3% to 42.5%.

Apoptosis Analysis[3]

Cell 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%).
体内研究
(In Vivo)

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[1].
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[3].

Animal Model:Type II collagen-induced arthritis (CIA) in DBA/1J mice[1]
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)[3]
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.
分子量

505.01

性状

Solid

Formula

C27H29ClN6O2

CAS 号

288250-47-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 5.5 mg/mL(10.89 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9802 mL9.9008 mL19.8016 mL
5 mM0.3960 mL1.9802 mL3.9603 mL
10 mM0.1980 mL0.9901 mL1.9802 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 0.5 mg/mL (0.99 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.99 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.5 mg/mL (0.99 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.99 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 0.5 mg/mL (0.99 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.99 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。