Semapimod
Based on 5 publication(s) in Google Scholar
Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders.
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- No. CAS: 352513-83-8
- Fòrmula: C34H52N18O2
- Peso molecular:744.90
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Semapimod
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Actividad biológica
Descripciòn
IC50 & Target
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CD40 |
IL-1β |
IL-6 |
p38 MAPK |
In Vitro
Semapimod 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 completely abrogated nitric oxide production within the tunica muscularis[2].
Semapimod 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 desensitizes TLR signaling via its effect on the TLR chaperone gp96[3].
Semapimod (0-500 nM) inhibits microglia-stimulated GL261 invasion[4].
Semapimod (0-10 µM) dose not affect serum-stimulated glioblastoma cell invasion, even at 10 µM, underlining the selectivity of semapimod for cells from the monocytic lineage[4].
Semapimod (200 nM) does not affect microglia-stimulated glioblastoma cell proliferation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Semapimod restores AM-induced akt phosphorylation and cGMP production in OZ rats[1].
Semapimod (6 mg/kg/day, Intracranially for 1 week) inhibits glioblastoma cell invasion in vivo[4].
Semapimod (intracranially administered, 2 weeks) semapimos strongly increases the survival of GL261 tumor-bearing animals in combination with radiation, but has no significant benefit in the absence of radiation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male OZ rats[1]
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Dosage:5 mg/kg
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Administration:I.p; daily for 2 weeks
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Result:Restored endothelium-dependent vasorelaxation in OZ rats.
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Animal Model:C57Bl/6 mice (GL261 cells were orthotopically implanted)[4]
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Dosage:6 mg/kg/day
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Administration:Intracranially for 1 week, delivered via an osmotic pump
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Result:Inhibited tumor cell invasion by more than 75%.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 352513-83-8
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Peso molecular 744.90
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Fòrmula C34H52N18O2
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SMILES
O=C(NC1=CC(/C(C)=N/NC(N)=N)=CC(/C(C)=N/NC(N)=N)=C1)CCCCCCCCC(NC2=CC(/C(C)=N/NC(N)=N)=CC(/C(C)=N/NC(N)=N)=C2)=O
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Synonyms
CNI-1493 free base; CPSI-2364
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
Pureza y Documentación
Referencias
[1]. Nishimatsu H, et al. Blockade of endogenous proinflammatory cytokines ameliorates endothelial dysfunction in obese Zucker rats. Hypertens Res. 2008;31(4):737‐743. [Content Brief]
[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. [Content Brief]
[3]. Wang J, et al. Experimental Anti-Inflammatory Drug Semapimod Inhibits TLR Signaling by Targeting the TLR Chaperone gp96. J Immunol. 2016;196(12):5130‐5137. [Content Brief]
[4]. Miller IS, et al. Semapimod sensitizes glioblastoma tumors to ionizing radiation by targeting microglia. PLoS One. 2014 May 9;9(5):e95885. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Semapimod Related Classifications
HY-15509 Related Classifications
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