Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy-
![Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy- Structure](CAS/20210305/GIF/2543545-44-2.gif)
- CAS No.
- 2543545-44-2
- Chemical Name:
- Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy-
- Synonyms
- LT052;LT052,LT-052;Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy-
- CBNumber:
- CB49786709
- Molecular Formula:
- C22H19N5O4S
- Molecular Weight:
- 449.48
- MDL Number:
- MOL File:
- 2543545-44-2.mol
Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy- Properties
| Boiling point | 759.4±70.0 °C(Predicted) |
|---|---|
| Density | 1.49±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO : 10.42 mg/mL (23.18 mM; Need ultrasonic) |
| pka | 6.87±0.20(Predicted) |
| form | Solid |
| color | Yellow to orange |
Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy- Chemical Properties,Uses,Production
Biological Activity
LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research[1]. LT052 (1 μM) inhibits NF-κB transcriptional activity in HUVECs cells and inhibit nitric oxide (NO) production (inhibition rate: 101.89%) in RAW264.7 cells. In the evaluation of in vitro inflammatory activity, LT052 maintains comparable or better anti-inflammatory activity than the pan-BET inhibitor (JQ1) compared to the protein weak activity[1].LT052 displays the highinhibitory activity against BRD4(1) (IC50: 87.7±4.9 nM), BRD3(1) (IC50: 246.3±20.2 nM), and BRDT(1) (IC50: 357.1±8.3 nM). LT052 also has inhibitory activities against BRPF1b (IC50: 567.5±16.9 nM). Additionlly, LT052 shows a 238-fold selectivity toward BD1 over BD2 with Kd of 105 nM and >25 μM for BD1 and BD2, respectively[1].LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways[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].LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway[1].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].
References
[1]. Jiang F, et al. Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis. J Med Chem. 2019 Dec 26;62(24):11080-11107.
Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy- Preparation Products And Raw materials
Raw materials
Preparation Products
Benzenesulfonamide, N-[1,2-dihydro-1-methyl-4-(4-methyl-1H-imidazol-1-yl)-2-oxopyrrolo[4,3,2-de]quinolin-6-yl]-2-methoxy- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49391 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Yujinpharma(Tianjin) Technology Co.,Ltd. | 13370351217 kungfu1217@1 | kungfu1217@163.com | China | 9429 | 58 |
| Birdo (Shanghai) Medical Technology Co., Ltd. | 021-021-021-58099077-8102-8041-8041 18601625411 | sales@birdotech.com | China | 8892 | 58 |
| Taizhou Nanfeng Pharmaceutical Research Institute | 18616377689 | nanfengdrug@163.com | China | 20566 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |