Semapimod tetrahydrochloride (Synonyms:CNI-1493; CPSI-2364 tetrahydrochloride)
目录号 : KM8523 CAS No. : 164301-51-3 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
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生物活性

Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.

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 (IC50≈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.
分子式
C34H52N18O2.4ClH
分子量
890.74
CAS号
164301-51-3
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

H2O : 14.29 mg/mL (16.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1227 mL 5.6133 mL 11.2266 mL
5 mM 0.2245 mL 1.1227 mL 2.2453 mL
10 mM 0.1123 mL 0.5613 mL 1.1227 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

临床试验
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