C004019
Based on 1 Customer Validation
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: Tau Protein ligand (HY-138679); Blue: VHL ligand (HY-138678); Black: linker (HY-140189)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.72%
- CAS 番号: 2417159-57-8
- 分子式: C49H70N12O9S2
- 分子量:1035.29
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保管条件:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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.
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Cell Line:HEK293-hTau cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM and 20 μM
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Incubation Time:24 h
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Result:Induced a concentration-dependent reduction of total tau (Tau5) and tau phosphorylated (p-tau) at multiple AD-related sites (pS214, pS262, pS396, pS404).
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.
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Animal Model:hTau transgenic mice aged 12 months old[1]
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Dosage:3 mg/kg
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Administration:Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
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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.
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Animal Model:3xTg-AD mice aged 9.5 months old[1]
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Dosage:3 mg/kg
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Administration:Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
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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.
化学情報
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CAS 番号 2417159-57-8
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性状 Solid
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分子量 1035.29
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分子式 C49H70N12O9S2
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Color White to off-white
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 |
C004019 関連分類
HY-138669 関連分類
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