LT052

未知

LT052

L647401-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

LT052 is a highly selective BET BD1 inhibitor with an IC 50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC 50 =12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research In Vitro 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) (IC 50 : 87.7±4.9 nM), BRD3(1) (IC 50 : 246.3±20.2 nM), and BRDT(1) (IC 50 : 357.1±8.3 nM). LT052 also has inhibitory activities against BRPF1b (IC 50 : 567.5±16.9 nM). Additionlly, LT052 shows a 238-fold selectivity toward BD1 over BD2 with K d 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:BRD4 BD1 87.7 nM (IC 50 ) BRD3 BD1 246.3 nM (IC 50 ) BRDT BD1 357.1 nM (IC 50 ) BRPF1b 567.5 nM (IC 50 )

LT052 是一种高选择性 BET BD1 抑制剂，IC 50 为 87.7 nM。LT052 对 BRD4 BD1 具有纳摩尔效力，对 BRD4 BD2 具有 138 倍的选择性（IC 50 =12.130 μM）。LT052 具有抗炎活性，可用于急性痛风关节炎的再治疗。

2543545-44-2

C22H19N5O4S

449.48 g/mol

145925666

CC1=CN(C=N1)C2=NC3=C(C=CC4=C3C(=C2)C(=O)N4C)NS(=O)(=O)C5=CC=CC=C5OC

2-methoxy-N-[2-methyl-6-(4-methylimidazol-1-yl)-3-oxo-2,7-diazatricyclo[6.3.1.04,12]dodeca-1(12),4,6,8,10-pentaen-9-yl]benzenesulfonamide

1S/C22H19N5O4S/c1-13-11-27(12-23-13)19-10-14-20-16(26(2)22(14)28)9-8-15(21(20)24-19)25-32(29,30)18-7-5-4-6-17(18)31-3/h4-12,25H,1-3H3

FSMTUHGXWGJNKK-UHFFFAOYSA-N

CC1=CN(C=N1)C2=NC3=C(C=CC4=C3C(=C2)C(=O)N4C)NS(=O)(=O)C5=CC=CC=C5OC

145925666

DMSO : 10.42 mg/mL (23.18 mM; Need ultrasonic)