PROTAC α-Synuclein/Tau degrader 1

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

Cat. No.: HY-157839 Purity: 99.28%: Data Sheet
COA

SDS
Handling Instructions
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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)).

For research use only. We do not sell to patients.

PROTAC α-Synuclein/Tau degrader 1 Chemical Structure

CAS No. : 3032208-24-2

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

α-synuclein

1.57 μM (DC₅₀)

Cereblon

In Vitro

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.

In Vivo

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.

Molecular Weight

729.80

Formula

C₃₇H₃₉N₅O₉S

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.28%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

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

Handling Instructions (2659 KB)

References

[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