Art. -Nr.: HY-161723

LH2-051

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LH2-051, a lysosome-enhancing compound (LYEC), is a brain-penetrant dopamine transporter (DAT) inhibitor (K_i: 0.95 μM). LH2-051 inhibits DAT-mediated dopamine uptake with an IC₅₀ of 3.0 μM. LH2-051 promotes nuclear translocation of TFEB and lysosome biogenesis. LH2-051 improves the memory of amyloid precursor protein (APP)/Presenilin 1 (PS1) mice. LH2-051 can be used for the study of Alzheimer’s disease.

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Reinheit: 99.85%
CAS. Nr.: 2358754-22-8
Formel: C₂₇H₃₄N₂O₃
Molecular Weight:434.57

Speicherung:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

LH2-051 Chemical Structure

CAS. Nr.: 2358754-22-8

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

LH2-051 (3-50 μM, 3-12 h) promotes nuclear translocation of TFEB which is independent of inactivation of mTORC1 or GSK3β^[1].
LH2-051 (10^-4-10^-1 μM) binds directly to DAT (K_i = 0.95 μM) and inhibits DAT-mediated dopamine uptake with an IC₅₀ of 3.0 μM in HEK293 cells^[1].
LH2-051 (30 μM, 0-6 h) promotes lysosome biogenesis in HeLa cells and SH-SY5Y cells, which is regulated by CDK9-mediated phosphorylation of TFEB^[1].
LH2-051 (30 μM, 3 h) induces the translocation of DAT from the plasma membrane onto lysosomal membranes in SH-SY5Y cells^[1].

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

Immunofluorescence^[1]

Cell Line:

HeLa cells and SH-SY5Y cells
Concentration:

3, 5, 10, 30, 50 μM
Incubation Time:

3, 6 h
Result:

Promoted the nuclear translocation of TFEB-EGFP in a dose- and time-dependent manner.
Enhanced the staining and protein level of endogenous lysosomal-associated membrane protein 1 (LAMP1).
Enhanced the staining of Boron dipyrromethene difluoride (BODIPY) pepstatin A, which binds to active cathepsin D inside lysosomes.
Promoted translocation of endogenous DAT to lysosomes, and release of both endogenous CDK9 and endogenous TFEB from lysosomes.

Western Blot Analysis^[1]

Cell Line:

HeLa cells
Concentration:

30 μM
Incubation Time:

6 h
Result:

Induced translocation of endogenous TFEB from the cytosol into the nucleus.
Did not inhibit mTORC1 activity.
Did not significantly affect GSK3β phosphorylation at Ser9.

Real Time qPCR^[1]

Cell Line:

HeLa cells and TFEB KO cells
Concentration:

30 μM
Incubation Time:

12 h
Result:

Increased the expression of lysosomal and autophagic genes which was dependent on TFEB. protein 1 (LAMP1).
Enhanced the staining of Boron dipyrromethene difluoride (BODIPY) pepstatin A, which binds to active cathepsin D inside lysosomes.
Promoted translocation of endogenous DAT to lysosomes, and release of both endogenous CDK9 and endogenous TFEB from lysosomes.

Western Blot Analysis^[1]

Cell Line:

SH-SY5Y cells
Concentration:

30 μM
Incubation Time:

1, 2, 3, 6 h
Result:

Reduced the phosphorylation of Rpb1.

Parmacokinetics

Species	Dose	Route	T_max	T_1/2	C_max	AUC_0-t	AUC_0-∞	F	CL
Mice^[1]	10 mg/kg	i.p.	0.18 h	0.97 h	620 ng/mL	609 ng·h/mL	613 ng·h/mL	50.4 %	/
Mice^[1]	5 mg/kg	i.v.	/	0.95 h	/	604 ng·h/mL	607 ng·h/mL	50.4 %	140 mL/min/kg

In Vivo

LH2-051 (10 mg/kg, i.p., once daily, 30 days) alleviates AD-like symptoms in APP/PS1 mice^[1].

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

Animal Model:

Five-month-old APP/PS1 mice (male)^[1]
Dosage:

10 mg/kg
Administration:

i.p. once daily for 30 days
Result:

Reduced Aβ load by 63.2% in the cortex and 65.6% in hippocampus compared with age-matched vehicle-injected controls.
Upregulated the expression of lysosomal and autophagic genes in APP/PS1 mouse brains.
Took significantly less time to locate the hidden platform and landed on the platform more often when compared to vehicle-injected controls during the training trial.
Enhanced lysosome biogenesis and Aβ clearance in APP/PS1 mice, and improved their learning, memory, and cognitive function.

Chemical Information

CAS. Nr. 2358754-22-8
Appearance Solid
Molecular Weight 434.57
Formel C₂₇H₃₄N₂O₃
Color Off-white to light brown
SMILES

COC1=C(OC)C=C(C(CCC2=CNC3=C2C=CC=C3)N(CC4CCOCC4)CC5)C5=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (230.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3011 mL

11.5056 mL

23.0113 mL

5 mM

0.4602 mL

2.3011 mL

4.6023 mL

10 mM

0.2301 mL

1.1506 mL

2.3011 mL

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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (5.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yin L, et al. Inhibition of the dopamine transporter promotes lysosome biogenesis and ameliorates Alzheimer's disease-like symptoms in mice. Alzheimers Dement. 2023 Apr;19(4):1343-1357. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3011 mL	11.5056 mL	23.0113 mL	57.5281 mL
	5 mM	0.4602 mL	2.3011 mL	4.6023 mL	11.5056 mL
	10 mM	0.2301 mL	1.1506 mL	2.3011 mL	5.7528 mL
	15 mM	0.1534 mL	0.7670 mL	1.5341 mL	3.8352 mL
	20 mM	0.1151 mL	0.5753 mL	1.1506 mL	2.8764 mL
	25 mM	0.0920 mL	0.4602 mL	0.9205 mL	2.3011 mL
	30 mM	0.0767 mL	0.3835 mL	0.7670 mL	1.9176 mL
	40 mM	0.0575 mL	0.2876 mL	0.5753 mL	1.4382 mL
	50 mM	0.0460 mL	0.2301 mL	0.4602 mL	1.1506 mL
	60 mM	0.0384 mL	0.1918 mL	0.3835 mL	0.9588 mL
	80 mM	0.0288 mL	0.1438 mL	0.2876 mL	0.7191 mL
	100 mM	0.0230 mL	0.1151 mL	0.2301 mL	0.5753 mL

Keywords

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LH2-051

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Anti-Aging Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LH2-051

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Anti-Aging Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LH2-051 Related Classifications

HY-161723 Related Classifications