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产品总数：60957
| 中文名称 |
Semapimod tetrahydrochloride
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| 英文名称 |
Semapimod tetrahydrochloride
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| 英文别名 |
Decanediamide,N1,N10-bis[3,5-bis[1-[2-(aminoiminomethyl)hydrazinylidene]ethyl]phenyl]-,hydrochloride (1:4);N,N'-bis[3,5-bis[(E)-N-(diaminomethylideneamino)-C-methylcarbonimidoyl]phenyl]decanediamide,tetrahydrochloride;AXD 455;CNI 1493;Decanediamide, N,N'-bis(3,5-bis(1-((aminoiminomethyl)hydrazono)ethyl)phenyl)-, tetrahydrochloride;N,N'-Bis(3,5-bis(1-((aminoiminomethyl)hydrazono)ethyl)phenyl)decanediamide tetrahydrochloride;Semapimod HCl;Semapimod hydrochloride;Semapimod tetrahydrochloride
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| Cas No. |
164301-51-3
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| 分子式 |
C34H52N18O2.4ClH
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| 分子量 |
890.74
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| 包装储存 |
-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)
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| 产品详情 |
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。
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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 (IC 50 ≈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.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IL-1β IL-6
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| 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.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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 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.
Semapimod tetrahydrochloride restores AM-induced akt phosphorylation and cGMP production in OZ rats. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| ClinicalTrial |
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| 参考文献 |
[1]. Nishimatsu H, et al. Blockade of endogenous proinflammatory cytokines ameliorates endothelial dysfunction in obese Zucker rats. Hypertens Res. 2008;31(4):737‐743.[2]. Wehner S, Set al. Inhibition of p38 mitogen-activated protein kinase pathway as prophylaxis of postoperative ileus in mice. Gastroenterology. 2009;136(2):619‐629.
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| 溶解度数据 |
In Vitro: H2O : 2.17 mg/mL (2.44 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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