Y-320|cas:288250-47-5|西域试剂

Y-320,99.39%

产品编号：Bellancom-15898| CAS NO：288250-47-5| 分子式：C₂₇H₂₉ClN₆O₂| 分子量：505.01

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15898	￥1050.00	杭州北京（现货）
Bellancom-15898	￥1500.00	杭州北京（现货）
Bellancom-15898	￥5100.00	杭州北京（现货）
Bellancom-15898	￥8700.00	杭州北京（现货）

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Y-320

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 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC₅₀ values 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 of Paclitaxel (HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

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

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	1.9802 mL	9.9008 mL	19.8016 mL
5 mM	0.3960 mL	1.9802 mL	3.9603 mL
10 mM	0.1980 mL	0.9901 mL	1.9802 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 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。