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LT052
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Catalog No. T11887Cas No. 2543545-44-2
Alias LT 052
LT052 is a selective and efficient BET BD1 inhibitor with anti-inflammatory activity. It mediates the BRD4/NF-κB/NLRP3 inflammatory signaling pathway and can be used in gout arthritis research.
LT052
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Purity: 98.82%
Catalog No. T11887Alias LT 052Cas No. 2543545-44-2
LT052 is a selective and efficient BET BD1 inhibitor with anti-inflammatory activity. It mediates the BRD4/NF-κB/NLRP3 inflammatory signaling pathway and can be used in gout arthritis research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $34 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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:98.82%
Appearance:Solid
Color:Orange
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | LT052 is a selective and efficient BET BD1 inhibitor with anti-inflammatory activity. It mediates the BRD4/NF-κB/NLRP3 inflammatory signaling pathway and can be used in gout arthritis research. |
| Targets&IC50 | BRD3 BD1:246.3 nM, BRPF1b:567.5 nM, BRDT BD1:357.1 nM, BRD4 BD1:87.7 nM |
| In vitro | LT052 (1 μm,1h) inhibited MSU-induced apoptosis of THP-1 cells through the BRD4/NF-κB/NLRP3 signaling pathway. LT052 showed good inhibitory activity on NO production in RAW264.7 cells. LT052 inhibits NF-κB transcriptional activity in HUVECs. LT052 inhibits scorch death of macrophages in rat synovial tissue by regulating the BRD4/NF-κB/NLRP3 signaling pathway. [1] |
| In vivo | LT052 has a high clearance rate in the range of 93.517 µL/min/mg proteins to 146.685 µL/min/mg proteins in liver microsomes of multiple species (human, monkey, dog, rat). Overall, LT052 exhibits moderately stable levels of in vitro liver microsomal metabolism[1]. LT052 (1 mg/kg; intra-articular) suppresses synovial hyperplasia as well as severe neutrophil infiltration, and has a good therapeutic effect on MSU-induced acute gouty arthritis[1]. |
| Synonyms | LT 052 |
| Molecular Weight | 449.48 |
| Formula | C22H19N5O4S |
| Cas No. | 2543545-44-2 |
| Smiles | O=C1C2=CC(=NC3=C(C=CC(=C32)N1C)NS(=O)(=O)C=4C=CC=CC4OC)N5C=NC(=C5)C |
| Relative Density. | 1.49 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (11.12 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 μL PEG300 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 ddH2O 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.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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