产品
编 号：F715555
分子式：C22H19N5O4S
分子量：449.48
分子式：C22H19N5O4S
分子量：449.48
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2543545-44-2
产品详情
生物活性：
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.
体内研究：
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.LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway.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.Animal Model:Male Adult Sprague-Dawley rats (250-280 g) (acute gouty arthritis animal models)
Dosage:1 mg/kg
Administration:Intra-articular injection
Result:Restored the joint circumference to normal level.
体外研究：
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.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.LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways.
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.
体内研究：
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.LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway.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.Animal Model:Male Adult Sprague-Dawley rats (250-280 g) (acute gouty arthritis animal models)
Dosage:1 mg/kg
Administration:Intra-articular injection
Result:Restored the joint circumference to normal level.
体外研究：
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.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.LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备