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LT052
🥰Excellent
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
🥰Excellent
Purity: 98.87%
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 | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,490 | In Stock | |
| 50 mg | $2,480 | In Stock |
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CitedSelect Batch
Purity:98.87%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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, BRDT BD1:357.1 nM, BRD4 BD1:87.7 nM, BRPF1b:567.5 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]. |
| Alias | 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 & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (11.12 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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