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Semapimod tetrahydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Semapimod tetrahydrochloride图片
CAS NO:164301-51-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
CNI-1493
CPSI-2364 tetrahydrochloride
产品介绍
Semapimod tetrahydrochloride (CNI-1493) 是促炎细胞因子产生 (proinflammatory cytokine) 的抑制剂,可抑制TNF-αIL-1βIL-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。
生物活性

Semapimod tetrahydrochloride (CNI-1493), an inhibitor ofproinflammatory cytokineproduction, can inhibitTNF-α,IL-1β, andIL-6. Semapimod tetrahydrochloride inhibitsTLR4signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibitsp38 MAPKand nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders[1][2][3].

IC50& Target

IL-1β

 

IL-6

 

p38 MAPK

 

体外研究
(In Vitro)

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[2].
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[3].

体内研究
(In Vivo)

Semapimod tetrahydrochloride (5 mg/kg; i.p; daily for 2 weeks) ameliorates endothelial dysfunction in Obese Zucker (OZ) rats[1].
Semapimod tetrahydrochloride restores AM-induced akt phosphorylation and cGMP production in OZ rats[1].

Animal Model:Male OZ rats[1]
Dosage:5 mg/kg
Administration:I.p; daily for 2 weeks
Result:Restored endothelium-dependent vasorelaxation in OZ rats.
Clinical Trial
分子量

890.74

性状

Solid

Formula

C34H56Cl4N18O2

CAS 号

164301-51-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

H2O : 2.17 mg/mL(2.44 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.1227 mL5.6133 mL11.2266 mL
5 mM---------
10 mM---------
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。