Resatorvid
作者：齐岳
发布时间：2023-09-12
09:05:17
点击数：
产品名称：Resatorvid
产品描述：
| 产品描述 | Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid inhibits IL-6, TNF-R and NO production (IC50s: 1.3 nM, 1.9 nM, and 1.8 nM). |
| 靶点活性 | NO:1.8 nM , IL-6:1.3 nM , TNF-R:1.9 nM |
| 体外活性 | Resatorvid suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs, IC50s: 11-33 nM). Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM. Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells [1]. |
| 体内活性 | In ApoE knockout and wild-type mice, Resatorvid (0.3?mg/kg; intraperitoneal injection; twice a week; for 4 weeks) treatment inhibits serum autoantibodies (ANA and anti-dsDNA), cytokines (IFN-γ, TNF-α, IL-1β), lung inflammation, and intima-media thickness in brachiocephalic artery [2]. |
| 细胞实验 | Cell Line: RAW264.7 cells. Concentration: 1 nM, 10 nM, 100 nM. Incubation Time: 4 hours [1] |
| 动物实验 | Animal Model: 30 ApoE knockout and 30 wild-type mice on a C57BL/6 background (female, 10 weeks old). Dosage: 0.3?mg/kg. Administration: i.p.; twice a week; for 4 weeks [3] |
| 别名 | TAK-242, 瑞沙托维, CLI-095 |
| 分子量 | 361.82 |
| 分子式 | C15H17ClFNO4S |
| CAS No. | 243984-11-4 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: Insoluble
DMSO: 100 mg/mL (276.38 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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