PROTAC α-Synuclein/Tau degrader 1

Name: PROTAC α-Synuclein/Tau degrader 1
Brand: MedChemExpress
SKU: HY-157839
Rating: 4.5 (0 reviews)

製品番号: HY-157839 純度: 99.28%: Data Sheet SDS COA 取扱説明書
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PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC₅₀ of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with K_Ds of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)).

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。

PROTAC α-Synuclein/Tau degrader 1 構造式

CAS 番号 : 3032208-24-2

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 409	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 409	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$255	在庫あり	Estimated Time of Arrival: December 31
10 mg	$405	在庫あり	Estimated Time of Arrival: December 31
25 mg	$810	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1300	在庫あり	Estimated Time of Arrival: December 31
100 mg		お問い合わせ
200 mg		お問い合わせ

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カスタマーレビュー

Based on 0 publication(s) in Google Scholar

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

α-synuclein 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

α-synuclein α-synuclein Aggregation α-synuclein/CHMP2B

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

α-synuclein

1.57 μM (DC₅₀)

Cereblon

体外実験

PROTAC α-Synuclein/Tau degrader 1 (Compound T4) (5 μM, 24 h) inhibit the α-Syn aggregate-mediated ROS generation and ΔΨm loss and protect SH-SY5Y Cells from α-Syn aggregate-associated toxicity^[1].

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

体内実験

PROTAC α-Synuclein/Tau degrader 1 (Compound T4) (2-8 mg/kg, i.v., once daily for 7 days) significantly alleviates the symptoms of the parkinson's disease mice^[1].
PROTAC α-Synuclein/Tau degrader 1 (8 mg/kg, i.v., single dose) shows good half-life in both plasma (AUC_0-24h = 109.21 μM·h, t_1/2 = 3.24 h) and brain tissues (AUC_0-24h = 6.02 μM·h, t_1/2 = 4.21 h) in C57BL/6 mice and the absorption, distribution, metabolism, and excretion (ADME) properties in SD rats are basically consistent^[1].

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

Animal Model:	MPTP (HY-15608)-induced PD model established in Male C57BL/6 mice (60-70 days old, weighed 22-24 g) ^[1]
Dosage:	2, 4, and 8 mg/kg
Administration:	Intravenous injection (i.v.), once daily for 7 days
Result:	Significantly reduced midbrain α-Syn aggregates (reduced by 78%) and total tau in the hippocampus (decreased by 61%). Reduced the area of α-Syn-positive cells in the SNc region by 72%. Increased the survival rate of dopamine neurons by 65%. No abnormalities at 8 mg/kg and only a slight increase in ALT/AST was observed at 80 mg/kg.

分子量

729.80

分子式

C₃₇H₃₉N₅O₉S

CAS 番号

3032208-24-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(OCC(NCCOCCOCCOCCNC4=CC=C(C(S5)=NC6=C5C=C(C)C=C6)C=C4)=O)=C3C1=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (137.02 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	1.3702 mL	6.8512 mL	13.7024 mL
5 mM	0.2740 mL	1.3702 mL	2.7405 mL
10 mM	0.1370 mL	0.6851 mL	1.3702 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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）

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濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 99.28%

Select Batch:

データシート (275 KB) SDS (252 KB)

COA (251 KB) HNMR (263 KB) RP-HPLC (266 KB) LCMS (88 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Wentao Zhu, et al. Discovery of Effective Dual PROTAC Degraders for Neurodegenerative Disease-Associated Aggregates. J Med Chem. 2024 Feb 14. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3702 mL	6.8512 mL	13.7024 mL	34.2560 mL
	5 mM	0.2740 mL	1.3702 mL	2.7405 mL	6.8512 mL
	10 mM	0.1370 mL	0.6851 mL	1.3702 mL	3.4256 mL
	15 mM	0.0913 mL	0.4567 mL	0.9135 mL	2.2837 mL
	20 mM	0.0685 mL	0.3426 mL	0.6851 mL	1.7128 mL
	25 mM	0.0548 mL	0.2740 mL	0.5481 mL	1.3702 mL
	30 mM	0.0457 mL	0.2284 mL	0.4567 mL	1.1419 mL
	40 mM	0.0343 mL	0.1713 mL	0.3426 mL	0.8564 mL
	50 mM	0.0274 mL	0.1370 mL	0.2740 mL	0.6851 mL
	60 mM	0.0228 mL	0.1142 mL	0.2284 mL	0.5709 mL
	80 mM	0.0171 mL	0.0856 mL	0.1713 mL	0.4282 mL
	100 mM	0.0137 mL	0.0685 mL	0.1370 mL	0.3426 mL