1. Apoptosis
  2. RIP kinase
  3. SZM679

SZM679 是一种口服有效的选择性 RIPK1 抑制剂,对 RIPK1 和 RIPK3 的 Kd 值分别为 8.6 nM 和 >5000 nM。SZM679 逆转肿瘤坏死因子诱导的全身炎症反应。SZM679 可降低海马和皮质中 Tau 蛋白的过度磷酸化、神经炎症和 RIPK1 磷酸化水平。SZM679 可用于阿尔茨海默病 (AD) 的研究。

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SZM679 Chemical Structure

SZM679 Chemical Structure

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规格 价格 是否有货 数量
5 mg ¥5184
In-stock
10 mg ¥8264
In-stock
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100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD)[1].

IC50 & Target[1]

RIPK1

8.6 nM (Kd)

RIPK3

>5000 nM (Kd)

体外研究
(In Vitro)

SZM679 (0-10 μM; 24 h; necrotic L929 and HT-29 cells) has an anti-necrosis activity by Inhibiting the RIPK1 pathway with an EC50 value of 2 nM. SZM679 also protects against TNF-α, cycloheximide, and z-VAD-fmk (TCZ)-induced necroptosis. SZM679 protects against necroptosis induced by TZ in a dose dependent manner[1].
SZM679 (1 μM; 6 h; necrotic HT-29 cells) selectively inhibits the expression of RIPK1 but not RIPK3 or MLKL. SZM679 blocks necrosome formation by inhibiting TSZ-induced phosphorylation of RIPK1[1].

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

Western Blot Analysis[1]

Cell Line: Necrotic HT-29 cells
Concentration: 1 μM
Incubation Time: 6 hours
Result: Inhibited the phosphorylation of RIPK1 at 1 μM, resulting in the inhibition of the downstream phosphorylation of RIPK3 and MLKL.
体内研究
(In Vivo)

SZM679 (10-40 mg/kg; i.p.; male C57BL/6 J mice with TNF-induced SIRS models) protects against necroptosis-specific TNF-induced systemic inflammatory response syndrome (SIRS) in vivo[1].
SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) improves cognitive function in STZ-induced AD mice[1].
SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) rescues brain structure damage with no obvious toxicity and decreases AD biomarkers and decreases the expression levels of inflammatory cytokines and inhibits RIPK1 phosphorylation in the brain tissues of AD mice[1].

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

Animal Model: Male C57BL/6 J mice with TNF-induced SIRS models[1]
Dosage: 10, 20, and 40 mg/kg
Administration: Intraperitoneal injection
Result: Protected mice in a dose-dependent manner from hypothermia and death.
Animal Model: Male C57BL/6 J mice with AD models[1]
Dosage: 1 mg/kg
Administration: Administered intragastrically; once daily for 7 days
Result: Improved the anxiety, behavior, and exploratory ability of AD mice.
Improved the learning and memory ability of AD mice.
Animal Model: Male C57BL/6 J mice with AD models[1]
Dosage: 1 mg/kg
Administration: Administered intragastrically; once daily for 7 days
Result: Rescued the damaged hippocampal structure of AD mice and restored the cell number and morphology.
Down-regulated the expression of the inflammatory cytokines, the IL-1β and TNF-α levels.
分子量

591.51

Formula

C27H18F5N3O5S

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (211.32 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 1.6906 mL 8.4529 mL 16.9059 mL
5 mM 0.3381 mL 1.6906 mL 3.3812 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

SZM679 相关分类

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 1.6906 mL 8.4529 mL 16.9059 mL 42.2647 mL
5 mM 0.3381 mL 1.6906 mL 3.3812 mL 8.4529 mL
10 mM 0.1691 mL 0.8453 mL 1.6906 mL 4.2265 mL
15 mM 0.1127 mL 0.5635 mL 1.1271 mL 2.8176 mL
20 mM 0.0845 mL 0.4226 mL 0.8453 mL 2.1132 mL
25 mM 0.0676 mL 0.3381 mL 0.6762 mL 1.6906 mL
30 mM 0.0564 mL 0.2818 mL 0.5635 mL 1.4088 mL
40 mM 0.0423 mL 0.2113 mL 0.4226 mL 1.0566 mL
50 mM 0.0338 mL 0.1691 mL 0.3381 mL 0.8453 mL
60 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7044 mL
80 mM 0.0211 mL 0.1057 mL 0.2113 mL 0.5283 mL
100 mM 0.0169 mL 0.0845 mL 0.1691 mL 0.4226 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:
SZM679
目录号:
HY-151873
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