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

C004019 is a BBB-penetrable 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: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))

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C004019

C004019 構造式

CAS 番号 : 2417159-57-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1298 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1298 在庫あり
Solid
1 mg $312 在庫あり
5 mg $780 在庫あり
10 mg $1140 在庫あり
25 mg $1656 在庫あり
50 mg $2256 在庫あり
100 mg $3036 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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C004019 関連抗体

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PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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製品説明

C004019 is a BBB-penetrable 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: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))[1]

体外実験

C004019 (0.01-100 μM; 24 h) does not cause significant changes in the viability of HEK293 cells stably expressing wild-type full-length human tau (HEK293-hTau)[1].
C004019 (0.01-20 μM; 24 h) inhibits the expression of total tau (Tau5) and phosphorylated tau in HEK293-hTau and SH-SY5Y cells[1].

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

C004019 関連抗体

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).
体内実験

C004019 (intracerebroventricular injection; 5 μL; 200 μM; single dose) reduces the level of tau protein in the brains of wild-type and 3xTg-AD mice[1].
C004019 (subcutaneous injection; 3-15 mg/kg; single dose) effectively clears tau protein in the brains of wild-type mice[1].
C004019 (subcutaneous injection; 3 mg/kg; once every 6 days for five times) promotes tau clearance and improves cognitive and synaptic functions in hTau and 3xTg-AD mice[1].

MedChemExpress (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

分子式

C49H70N12O9S2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@H](C[C@@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCNC(CN(C4=NC(N5CCN(CCC5)C(C)=O)=NC(NCCC6=CC=CS6)=N4)C)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, protect from light

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

DMSO : 50 mg/mL (48.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.0966 mL 0.4830 mL 0.9659 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 99.72%

COA (248 KB) HNMR (147 KB) RP-HPLC (304 KB) LCMS (236 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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C004019 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品番号:
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