2. PROTAC Neuronal Signaling
  3. PROTACs Tau Protein
  4. C004019

C004019 是一种能透过血脑屏障的和靶向 tau 的小分子 PROTAC。C004019 可同时招募 tau 和 E3 连接酶，通过促进 tau 的泛素化和蛋白酶体依赖性的降解，有效清除 tau 蛋白，进而改善阿尔兹海默症 (AD) 小鼠的突触和认知功能。C004019 可用于 AD 及 tau 蛋白相关疾病研究。(Pink: AZD2858 (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))

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C004019 Chemical Structure

C004019 Chemical Structure

CAS No. : 2417159-57-8

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规格 价格 是否有货 数量
1 mg ￥2250
In-stock
5 mg ￥5460
In-stock
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100 mg   询价  

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Customer Review

C004019 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: AZD2858 (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))[1]

体外研究
(In Vitro)

C004019 (0.01-100 μM; 24 小时) 不会对稳定表达野生型全长人 tau 蛋白的 HEK293 细胞 (HEK293-hTau) 活力产生显著变化[1]。
C004019 (0.01-20 μM; 24 小时) 在 HEK293-hTau 和 SH-SY5Y 中，可抑制总 tau (Tau5) 和磷酸化 tau 的表达[1]。

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

C004019 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293-hTau cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM and 20 μM
Incubation Time: 24 h
Result: Induced a concentration-dependent reduction of total tau (Tau5) and tau phosphorylated (p-tau) at multiple AD-related sites (pS214, pS262, pS396, pS404).
体内研究
(In Vivo)

C004019 (侧脑室给药; 5 μL; 200 μM; 单剂量) 可降低野生型和 3xTg-AD 小鼠脑内 tau 蛋白水平[1]。
C004019 (皮下注射; 3-15 mg/kg; 单剂量) 可有效清除野生型小鼠脑内的 tau 蛋白[1]。
C004019 (皮下注射; 3 mg/kg; 6 天一次; 共五次) 可在 hTau 和 3xTg-AD 小鼠中，促进 tau 的清除，改善小鼠的认知和突触功能[1]。

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

Animal Model: hTau transgenic mice aged 12 months old[1]
Dosage: 3 mg/kg
Administration: Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
Result: Significantly reduced total and p-tau levels in the hippocampal extracts.
Reduced both soluble and insoluble tau, more efficiently to the tau in the soluble fraction.
Ameliorated cognitive functions and dentritic plasticity in hTau transgenic mouse model.
Animal Model: 3xTg-AD mice aged 9.5 months old[1]
Dosage: 3 mg/kg
Administration: Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
Result: Remarkably reduced both soluble and insoluble tau levels in hippocampal and cortex extracts, more efficiently to the tau in the soluble fraction.
Significantly reduced T22-positive tau in the soluble fraction.
Improved the cognitive and synaptic functions in 3xTg-AD mice.
分子量

1035.29

Formula

C49H70N12O9S2
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

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (48.30 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 0.9659 mL 4.8296 mL 9.6591 mL
5 mM 0.1932 mL 0.9659 mL 1.9318 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 (protect from light)。-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

只
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

C004019 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 (protect from light)。-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 0.9659 mL 4.8296 mL 9.6591 mL 24.1478 mL
5 mM 0.1932 mL 0.9659 mL 1.9318 mL 4.8296 mL
10 mM 0.0966 mL 0.4830 mL 0.9659 mL 2.4148 mL
15 mM 0.0644 mL 0.3220 mL 0.6439 mL 1.6099 mL
20 mM 0.0483 mL 0.2415 mL 0.4830 mL 1.2074 mL
25 mM 0.0386 mL 0.1932 mL 0.3864 mL 0.9659 mL
30 mM 0.0322 mL 0.1610 mL 0.3220 mL 0.8049 mL
40 mM 0.0241 mL 0.1207 mL 0.2415 mL 0.6037 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.

Keywords:

C0040192417159-57-8C 004019C-004019PROTACsTau ProteinHEK293SH-SY5Y3xTg-AD micehTau transgenic miceInhibitorinhibitorinhibit

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产品名称：
C004019
目录号：
HY-138669
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