化合物NLRP3-IN-10 T61392
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
500 mg | 2641826-39-1 | ¥6,870.00 | 询底价 |
100 mg | 2641826-39-1 | ¥3,320.00 | 询底价 |
50 mg | 2641826-39-1 | ¥1,980.00 | 询底价 |
10 mg | 2641826-39-1 | ¥663.00 | 询底价 |
200 mg | 2641826-39-1 | ¥4,390.00 | 询底价 |
1 mg | 2641826-39-1 | ¥185.00 | 询底价 |
5 mg | 2641826-39-1 | ¥397.00 | 询底价 |
25 mg | 2641826-39-1 | ¥1,330.00 | 询底价 |
1 mL | 2641826-39-1 | ¥491.00 | 询底价 |
Product Introduction
Bioactivity
英文名: NLRP3-IN-10
描述: NLRP3-IN-10 (ZVN26391) 是强效的 NLRP3 抑制剂,抑制 IL-1β 释放的 IC50 为 251.1 nM。NLRP3-IN-10 通过减弱 ASC 斑点形成来抑制 NLRP3炎症小体激活。
体外活性: NLRP3-IN-10 (compound 14c) (0.4, 1.6, 6.4 μM; 40 min) exerts remarkable inhibitory activity on NLRP3 inflammasome activation induced by LPS-MSU (12 h) in THP-1 cells in a dose-dependent manner [1]. NLRP3-IN-10 (0.1-6.4 μM; 1.5 h) shows no cytotoxicity against THP-1 cells and (0.1, and 0.4 μM; 40 min) avoids Nigericin -induced pyroptosis [1]. NLRP3-IN-10 (0.1, 0.2, and 0.4 μM; 40 min) reduces the processing of caspase-1 p20 and IL-1β, in supernatants in THP-1 cells in a dose-dependent manner [1]. NLRP3-IN-10 (3 μM and 5 μM; 40 min) decreases LPS-induced THF-α, and (0.2 μM and 0.8 μM; 40 min) reduces the rate of THP-1 cells with ASC specks, indicating ASC oligomerization interruptionsup>[1]. NLRP3 inflammasome is regarded as a two-step process, including priming and action. NLRP3-IN-10 (1, 10, and 100 μM; 40 min) suppresses LPS-induced NLRP3 priming through directly interacting with NLRP3 [1].
体内活性: NLRP3-IN-10 (compound 14c) (10 mg/kg; i.v.; single dose) reduces peritoneal neutrophil influx in mice and IL-1β in the spleen in the MSU-induced peritonitis in LPS-primed mouse model [1]. NLRP3-IN-10 (10, 30, 90 mg/kg; p.o.; single dose) exhibits extremely low exposure (14.6 23.53 μg·h/L), poor bioavailability (2.47 13.79%), and high plasma clearance (2201.58 5551.12 L/h/kg) after different doses for oral administration [1]. Pharmacokinetics of NLRP3-IN-10 in mouse [1] Route Dose (mg/kg) AUC 0-t (μg·h/L) CL (L/h/kg) C max (μg/L) T 1/2 (h) T max (h) F (%) IV 10 105.88 133.75 81.97 3.13 0.11 PO 10 14.60 2201.58 3.35 7.43 2.11 13.79 PO 30 15.84 2583.27 16.42 7.92 1.26 4.99 PO 90 23.53 5551.12 13.59 6.08 4.21 2.47 Animal Model: MSU-induced peritonitis in a LPS-primed mouse model (C57BL/6J mice, 7-week-old, male) [1] LPS: 1 mg/kg, i.p.; MSU: 100 mg/kg, i.v. Dosage: 10 mg/kg Administration: Intravenous injection; single dose Result: Significantly reduced IL-1β release in the spleen of mice after 6 h treatment. Significantly reduced the increase of peritoneal neutrophil influx compared with the control group.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 4.4 mg/mL (12.05 mM)
关键字: NLRP3-IN-10 | ZVN 26391 | ZVN-26391
相关产品: Bergenin | Emlenoflast sodium | Dapansutrile | L-Canavanine sulfate | NLRP3-IN-2 | 7,4'-Dihydroxyflavone | BMS986299 | Imperatorin | Nigericin sodium salt | Molsidomine
相关库: Anti-Cancer Compound Library | NF-κB Signaling Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途