1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  2. RAR/RXR NO Synthase
  3. MSU-42011

MSU-42011 是一种具有口服活性的类视黄醇 X 受体 (RXR) 激动剂。MSU-42011 可以有效抑制 iNOS 以及 p-ERK 蛋白水平的表达。MSU-42011 具有免疫调节和抗肿瘤活性。MSU-42011 可用于癌症的研究。

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MSU-42011 Chemical Structure

MSU-42011 Chemical Structure

CAS No. : 2456434-36-7

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10 mg ¥1520
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25 mg ¥2800
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50 mg ¥4480
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity[1].

体外研究
(In Vitro)

MSU-42011 (0-1 μM) 在 RAW264.7 巨噬细胞样细胞中抑制 iNOS 的IC50 值为 158 nM[1]
MSU-42011 (300 nM;8 h) 显示在 HepG2 细胞中对 SREBP 的低诱导效果[1]
MSU-42011 (0-5000 nM;24 h) 在 HepG2 细胞中可以激活 RXRα[1]

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

RT-PCR[1]

Cell Line: HepG2 liver cancer cells
Concentration: 300 nM
Incubation Time: 8 h
Result: SREBP expression ranged from no change to a 1.49-fold induction compared to the vehicle control
体内研究
(In Vivo)

MSU-42011 (25 mg/kg, 口服, 持续 12 周) 显著降低了 A/J 小鼠肺癌模型中肿瘤的数量、大小和总体肿瘤负荷。
与对照组相比,增殖活跃的细胞较少,并显示 p-ERK 显著降低[1]
MSU-42011 (25 mg/kg; 口服; 单剂量) 在 A/J 小鼠肺癌模型中与 C/P 联合用药,在减少肿瘤数量、肿瘤大小和总体肿瘤负荷方面最有效。
减少了肺中的巨噬细胞,增加了 CD8+T 细胞的活化标志物[1]
MSU42011 (100 mg/kg; PO; 单剂量) 减轻小鼠肺肿瘤模型中的肿瘤负荷[2]

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

Animal Model: A/J mice (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[1]
Dosage: 25 mg/kg
Administration: Oral administration; One week after, i.p. every other week for a total of 6 injections with Carboplatin (HY-17393) (50 mg/kg) and paclitaxel (15 mg/kg); for 12 weeks
Result: The number and size of detected lung surface tumors increased not in the treatment group
Combines with C/P was most effective in reducing tumor number (67% vs. control), tumor size (76% vs. control), and overall tumor burden (92% vs. control).
Animal Model: A/J lung cancer model (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[2]
Dosage: 100 mg/kg
Administration: Oral administration; After 2 weeks, each mouse was intraperitoneally injected with anti-PD1 and anti-PDL1 antibodies at a rate of 50 μg/mouse, twice a week for a total of 22 times
Result: Showed that an increase in the ratio of anti-tumor CD8 T cells to CD4, CD25 T cells resulted in a significant reduction in tumor volume compared to MSU42011 or anti-PD(L)1 antibody alone.
分子量

382.54

Formula

C24H34N2O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (326.76 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6141 mL 13.0705 mL 26.1411 mL
5 mM 0.5228 mL 2.6141 mL 5.2282 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6141 mL 13.0705 mL 26.1411 mL 65.3526 mL
5 mM 0.5228 mL 2.6141 mL 5.2282 mL 13.0705 mL
10 mM 0.2614 mL 1.3071 mL 2.6141 mL 6.5353 mL
15 mM 0.1743 mL 0.8714 mL 1.7427 mL 4.3568 mL
20 mM 0.1307 mL 0.6535 mL 1.3071 mL 3.2676 mL
25 mM 0.1046 mL 0.5228 mL 1.0456 mL 2.6141 mL
30 mM 0.0871 mL 0.4357 mL 0.8714 mL 2.1784 mL
40 mM 0.0654 mL 0.3268 mL 0.6535 mL 1.6338 mL
50 mM 0.0523 mL 0.2614 mL 0.5228 mL 1.3071 mL
60 mM 0.0436 mL 0.2178 mL 0.4357 mL 1.0892 mL
80 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8169 mL
100 mM 0.0261 mL 0.1307 mL 0.2614 mL 0.6535 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MSU-42011
目录号:
HY-153832
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