This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Semapimod
Catalog No. T79304 CAS
352513-83-8
Synonyms:
CPSI-2364, CNI-1493 free base
Semapimod is an inhibitor of proinflammatory cytokine production, capable of suppressing TNF-α, IL-1β, and IL-6. It hinders TLR4 signaling with an IC50 of approximately 0.3 μM, impedes p38 MAPK, and reduces nitric oxide production in macrophages. This compound shows promise for treating various inflammatory and autoimmune disorders [1] [2] [3].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
Semapimod is an inhibitor of proinflammatory cytokine production, capable of suppressing TNF-α, IL-1β, and IL-6. It hinders TLR4 signaling with an IC50 of approximately 0.3 μM, impedes p38 MAPK, and reduces nitric oxide production in macrophages. This compound shows promise for treating various inflammatory and autoimmune disorders [1] [2] [3].
In vitro
Semapimod induces a notable decrease in the phosphorylation of p38-MAPK, the pro-inflammatory gene expression of macrophage inflammatory protein-1alpha, interleukin-6, monocyte chemoattractant protein-1, and intercellular adhesion molecule-1 in macrophages, as well as reducing neutrophil infiltration. It completely abolishes nitric oxide production within the muscular layer [2]. Through its effect on the TLR co-chaperone protein gp96, Semapimod desensitizes TLR signaling. In vitro, Semapimod tetrahydrochloride inhibits the ATP binding and ATPase activity of gp96 (IC 50 ≈0.2-0.4 μM). This desensitization of TLR signaling is due to its impact on the TLR molecular co-chaperone gp96 [3]. Semapimod (0-500 nM) suppresses the invasion of GL261 stimulated by microglia [4]. However, Semapimod (0-10 µM) does not affect the invasion of glioma cells stimulated by serum, highlighting its selectivity for the monocytic lineage, even at concentrations as high as 10 µM [4]. Furthermore, at a concentration of 200 nM, Semapimod does not impact the proliferation of glioma cells stimulated by microglia [4].
In vivo
Semapimod at a dosage of 5 mg/kg administered intraperitoneally once daily for two weeks improved endothelial dysfunction in Obese Zucker (OZ) rats [1]. This compound restored adrenomedullin (AM)-induced phosphorylation of akt and production of cyclic guanosine monophosphate (cGMP) in these rats [1]. Additionally, Semapimod, at a concentration of 6 mg/kg/day delivered intracranially for one week, inhibited the invasion of glioblastoma cells in vivo [4]. When combined with radiotherapy, intracranial administration of Semapimod over two weeks significantly enhanced survival rates in GL261 tumor-bearing animals, with no marked benefit observed in the absence of radiotherapy [4].
Synonyms
CPSI-2364, CNI-1493 free base
Molecular Weight
744.9
Formula
C34H52N18O2
CAS No.
352513-83-8
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.