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164301-51-3

中文名稱(chēng) 5MG
英文名稱(chēng) CNI-1493
CAS 164301-51-3
更新日期 2024/11/07 22:28:50
分子式 C34H53ClN18O2
分子量 781.37
MOL 文件 164301-51-3.mol
164301-51-3 結(jié)構(gòu)式 164301-51-3 結(jié)構(gòu)式

基本信息

英文別名
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

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C, protect from light
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to yellow
5MG價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-15509ASemapimod tetrahydrochloride164301-51-35mg1900元
2024/11/08HY-15509ASemapimod tetrahydrochloride164301-51-310 mg3250元
2024/11/08HY-15509ASemapimod tetrahydrochloride164301-51-325 mg5500元

常見(jiàn)問(wèn)題列表

生物活性
Semapimod tetrahydrochloride (CNI-1493) 是促炎細(xì)胞因子產(chǎn)生 (proinflammatory cytokine) 的抑制劑,可抑制TNF-α、IL-1β 和 IL-6。Semapimod tetrahydrochloride 抑制巨噬細(xì)胞 p38 MAPK 和一氧化氮生成。Semapimod tetrahydrochloride 抑制 TLR4 信號(hào) (IC50≈0.3 μM)。Semapimod tetrahydrochloride 在多種炎癥和自身免疫性疾病中具有潛在的作用。
靶點(diǎn)

IL-1β

IL-6

TNF-α

p38 MAPK

體外研究

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.

體內(nèi)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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