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VU-1545

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Catalog No. T23514Cas No. 890764-63-3
Alias VU 1545

VU-1545 is mGlu5 positive allosteric modulator.

VU-1545

VU-1545

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Purity: 98.8%
Catalog No. T23514Alias VU 1545Cas No. 890764-63-3
VU-1545 is mGlu5 positive allosteric modulator.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$38In StockIn Stock
5 mg$60In StockIn Stock
10 mg$81In StockIn Stock
25 mg$139In StockIn Stock
50 mg$226In StockIn Stock
100 mg$363In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.8%
Appearance:Solid
Color:Yellow
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Product Introduction

VU-1545 AI Summary
VU-1545 demonstrates significant bioactivities across a range of biological targets and systems. It shows notable affinity for the mGluR5 receptor, with a Ki value of 160.0 nM, suggesting competitive binding, and an EC50 value of 9.6 nM in enhancing glutamate-induced calcium flux in rat astrocytes, indicating its modulatory effect on receptor signaling. In addition to mGluR5, VU-1545 exhibits various biopotencies, including moderate activity in mitochondrial dynamics, lipid storage modulation, strong inhibition against AmpC Beta-Lactamase, ELG1-dependent DNA repair, and delayed death inhibition of the malarial parasite plastid. It also shows potential as an inhibitor of Nrf2, TGF-b, Hepatitis C Virus (HCV), GLP-1 receptor inverse agonist, human TDP1, and stage-specific inhibition of Vaccinia Orthopoxvirus. In antiviral assays, VU-1545 inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells by 9.16% at 10 µM concentration after 48 hours and shows potential inhibition of SARS-CoV-2 3CL-Pro protease by -2.219% at 20 µM. It also demonstrates activity in reducing SARS-CoV-2 induced cytotoxicity in VERO-6 cells by 0.36% at 10 µM concentration after 48 hours. Further, VU-1545 shows an inhibitory effect on human HDAC6 enzymatic activity, with 73.61% inhibition using a commercial peptide substrate. It impacts cell viability variably in HEK293T and U2OS cell lines, promoting growth, whereas it has mixed effects on human fibroblast cells. VU-1545 also affects the thermal stability of different molecular domains, either stabilizing or destabilizing them to varying extents. Moreover, it is active in GPCR β-arrestin recruitment assays with multiple targets, including GPR119, APLNR, ADRB2, FPR2, GLP1R, CX3CR1, AGTR1, ADGRF1, S1PR1, C5AR1, FFAR4, GPR35, and ADRA2A, showing diverse levels of activation and inhibition. This broad spectrum of activity highlights VU-1545's potential as a versatile bioactive molecule with applications in various therapeutic areas..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
VU-1545 is mGlu5 positive allosteric modulator.
Targets&IC50
mGluR5:9.6 nM (EC50), mGluR5:156 nM (Ki)
SynonymsVU 1545
Chemical Properties
Molecular Weight402.38
FormulaC22H15FN4O3
Cas No.890764-63-3
Smiles[O-][N+](=O)c1ccc(cc1)C(=O)Nc1cc(nn1-c1ccccc1F)-c1ccccc1
Relative Density.1.34 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (124.26 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4852 mL12.4261 mL24.8521 mL124.2606 mL
5 mM0.4970 mL2.4852 mL4.9704 mL24.8521 mL
10 mM0.2485 mL1.2426 mL2.4852 mL12.4261 mL
20 mM0.1243 mL0.6213 mL1.2426 mL6.2130 mL
50 mM0.0497 mL0.2485 mL0.4970 mL2.4852 mL
100 mM0.0249 mL0.1243 mL0.2485 mL1.2426 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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