PROTAC α-synuclein degrader 5

Name: PROTAC α-synuclein degrader 5
Brand: MedChemExpress
SKU: HY-155021
Rating: 4.5 (1 reviews)

Cat. No.: HY-155021 Purity: 95.42%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC₅₀ of 7.51 μM and the highest degradation rate D_max of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research.

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

PROTAC α-synuclein degrader 5 Chemical Structure

CAS No. : 2781922-42-5

Size	Price	Stock	Quantity
1 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 972	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

PROTAC α-synuclein degrader 5 (Compound 2b) (0-40 μM, 48 hour) decreases the level of α-synuclein aggregates within the treatment period in preformed fibril (PFF) -seeding model cells^[1].
PROTAC α-synuclein degrader 5 (0-10 μM, 48 hour) degrades α-synuclein aggregates in a dose-dependent manner, as indicated by the reduced number and density of α-synuclein (+) punctate as well as the gradually declined fluorescence intensity^[1].

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

Western Blot Analysis^[1]

Cell Line:	Preformed fibril (PFF)-seeding model in HEK-293T cells
Concentration:	0-40 μM
Incubation Time:	0-48 hours
Result:	Decreased the level of α-synuclein aggregates within the treatment period. This kind of change became statistically significant by 3h and reached its plateau after 24h. Lowered the level of α-synuclein aggregates in model cells after treatment of 48 h.

Immunofluorescence^[1]

Cell Line:	HEK-293T cells
Concentration:	0-10 μM
Incubation Time:	48 hours
Result:	Degraded α-synuclein aggregates inadose-dependent manner, as indicated bythe reduced number and density of α-synuclein (+) punctae aswell asthe gradually declined fluorescence intensity.

Molecular Weight

767.78

Formula

C₃₉H₄₁N₇O₁₀

CAS No.

2781922-42-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCOCCOCCOCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)CNC4=CC(C5=CC(C6=CC7=C(C=C6)OCO7)=NN5)=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (130.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3025 mL	6.5123 mL	13.0246 mL
5 mM	0.2605 mL	1.3025 mL	2.6049 mL
10 mM	0.1302 mL	0.6512 mL	1.3025 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.75 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (244 KB) HNMR (527 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Yichen Tong, et.al. Discovery of Small-Molecule Degraders for Alpha-Synuclein Aggregates. Journal of Medicinal Chemistry 2023 66 (12), 7926-7942

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.3025 mL	6.5123 mL	13.0246 mL	32.5614 mL
	5 mM	0.2605 mL	1.3025 mL	2.6049 mL	6.5123 mL
	10 mM	0.1302 mL	0.6512 mL	1.3025 mL	3.2561 mL
	15 mM	0.0868 mL	0.4342 mL	0.8683 mL	2.1708 mL
	20 mM	0.0651 mL	0.3256 mL	0.6512 mL	1.6281 mL
	25 mM	0.0521 mL	0.2605 mL	0.5210 mL	1.3025 mL
	30 mM	0.0434 mL	0.2171 mL	0.4342 mL	1.0854 mL
	40 mM	0.0326 mL	0.1628 mL	0.3256 mL	0.8140 mL
	50 mM	0.0260 mL	0.1302 mL	0.2605 mL	0.6512 mL
	60 mM	0.0217 mL	0.1085 mL	0.2171 mL	0.5427 mL
	80 mM	0.0163 mL	0.0814 mL	0.1628 mL	0.4070 mL
	100 mM	0.0130 mL	0.0651 mL	0.1302 mL	0.3256 mL