1. MAPK/ERK Pathway
  2. MAPKAPK2 (MK2)
  3. Zunsemetinib

Zunsemetinib  (Synonyms: ATI-450; CDD-450)

目录号: HY-139553 纯度: 99.37% ee.: 100.00%
COA 产品使用指南

Zunsemetinib (CDD-450) 是一种具有口服活性的 p38α 丝裂原激活蛋白激酶激活蛋白激酶2 (MK2)通路抑制剂。Zunsemetinib 可用于免疫炎症性疾病的研究。

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Zunsemetinib Chemical Structure

Zunsemetinib Chemical Structure

CAS No. : 1640282-42-3

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1 mg ¥3400
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Customer Review

Other Forms of Zunsemetinib:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1].

IC50 & Target

MK2[1]

体外研究
(In Vitro)

Zunsemetinib (1 and 10 μM; 1 hour; WT and NOM ID BMMs) has no effect on NLRP3 expression, but decreases IL-1β expression by promoting IL-1β mRNA degradation[1].
Zunsemetinib (0.4 nM~1 μM; 16 hours; PBMC) reduces IL-1β secretion and promotes IL-1β mRNA instability[1].
Zunsemetinib selectively blocks p38α MAPK activation of the proinflammatory kinase MK2 while sparing p38α activation of other effectors such as PRAK and ATF2. Zunsemetinib inhibits in vitro osteoclast formation induced by RANKL[1].

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

RT-PCR[1]

Cell Line: WT and NOM ID BMMs
Concentration: 1 and 10 μM
Incubation Time: 1 hour
Result: Had no effect on NLRP3 expression, but decreased IL-1β expression by promoting IL-1β mRNA degradation.
体内研究
(In Vivo)

Zunsemetinib (1,000 ppm; p.o.) blocks LPS-induced TNF-α expression persisted for up to 4 weeks after dosing[1].
Zunsemetinib (10 and 20 mg/kg; p.o.) increases bone density[1].
Zunsemetinib prevents osteopenia in NOM IDc mice through inhibition of osteoclastogenesis[1].

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

Animal Model: 8-week-old WT female mice[1]
Dosage: 1,000 ppm
Administration: P.o.
Result: Blocked LPS-induced TNF-α expression persisted for up to 4 weeks after dosing.
Animal Model: Rats[1]
Dosage: 10 and 20 mg/kg
Administration: P.o.
Result: Increased bone density.
分子量

513.92

Formula

C25H22ClF2N5O3

CAS 号
性状

固体

颜色

White to yellow

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 : 100 mg/mL (194.58 mM; 超声助溶; 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 1.9458 mL 9.7291 mL 19.4583 mL
5 mM 0.3892 mL 1.9458 mL 3.8917 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

纯度: 99.37% ee.: 100.00%

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 1.9458 mL 9.7291 mL 19.4583 mL 48.6457 mL
5 mM 0.3892 mL 1.9458 mL 3.8917 mL 9.7291 mL
10 mM 0.1946 mL 0.9729 mL 1.9458 mL 4.8646 mL
15 mM 0.1297 mL 0.6486 mL 1.2972 mL 3.2430 mL
20 mM 0.0973 mL 0.4865 mL 0.9729 mL 2.4323 mL
25 mM 0.0778 mL 0.3892 mL 0.7783 mL 1.9458 mL
30 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6215 mL
40 mM 0.0486 mL 0.2432 mL 0.4865 mL 1.2161 mL
50 mM 0.0389 mL 0.1946 mL 0.3892 mL 0.9729 mL
60 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8108 mL
80 mM 0.0243 mL 0.1216 mL 0.2432 mL 0.6081 mL
100 mM 0.0195 mL 0.0973 mL 0.1946 mL 0.4865 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:
Zunsemetinib
目录号:
HY-139553
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