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164301-51-3

中文名称 5MG
英文名称 CNI-1493
CAS 164301-51-3
更新日期 2024/07/27 21:42:12
分子式 C34H53ClN18O2
分子量 781.37
MOL 文件 164301-51-3.mol
164301-51-3 结构式 164301-51-3 结构式

基本信息

英文别名
Semapimod hydrochloride
SeMapiMod (tetrahydrochloride)
Semapimod (tetrahydrochloride)(CNI-1493)
N,N'-bis[3,5-bis[(E)-N-(diaminomethylideneamino)-C-methylcarbonimidoyl]phenyl]decanediamide,tetrahydrochloride
N,N'-bis[3-[(E)-N-(diaminomethylideneamino)-C-methylcarbonimidoyl]-5-[(Z)-N-(diaminomethylideneamino)-C-methylcarbonimidoyl]phenyl]decanediamide:tetrahydrochloride

物理化学性质

储存条件-20°C, protect from light
溶解度溶于二甲基亚砜
形态Solid
颜色White to yellow
5MG价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-15509ASemapimod tetrahydrochloride164301-51-35mg1900元
2024/04/30HY-15509ASemapimod tetrahydrochloride164301-51-310 mg3250元
2024/04/30HY-15509ASemapimod tetrahydrochloride164301-51-325 mg5500元

常见问题列表

生物活性
Semapimod tetrahydrochloride (CNI-1493) 是促炎细胞因子产生 (proinflammatory cytokine) 的抑制剂,可抑制TNF-α、IL-1β 和 IL-6。Semapimod tetrahydrochloride 抑制巨噬细胞 p38 MAPK 和一氧化氮生成。Semapimod tetrahydrochloride 抑制 TLR4 信号 (IC50≈0.3 μM)。Semapimod tetrahydrochloride 在多种炎症和自身免疫性疾病中具有潜在的作用。
靶点

IL-1β

IL-6

TNF-α

p38 MAPK

体外研究

Semapimod tetrahydrochloride leads to a significant decrease of p38-MAPK phosphorylation in macrophages, proinflammatory gene expression of macrophage inflammatory protein-1alpha, interleukin-6, monocyte chemoattractant protein-1, and intercellular adhesion molecule-1, and neutrophil infiltration. Semapimod tetrahydrochloride completely abrogated nitric oxide production within the tunica muscularis.
Semapimod tetrahydrochloride desensitizes TLR signaling via its effect on the TLR chaperone gp96. Semapimod tetrahydrochloride inhibits ATP-binding and ATPase activities of gp96 in vitro (IC 50 ≈0.2-0.4 μM). Semapimod tetrahydrochloride desensitizes TLR signaling via its effect on the TLR chaperone gp96.

体内研究

Semapimod tetrahydrochloride (5 mg/kg; i.p; daily for 2 weeks) ameliorates endothelial dysfunction in Obese Zucker (OZ) rats.
Semapimod tetrahydrochloride restores AM-induced akt phosphorylation and cGMP production in OZ rats.

Animal Model: Male OZ rats
Dosage: 5 mg/kg
Administration: I.p; daily for 2 weeks
Result: Restored endothelium-dependent vasorelaxation in OZ rats.
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