Semapimod
Semapimod Basic information
- Product Name:
- Semapimod
- Synonyms:
-
- semapimod
- N,N'-Bis[3,5-bis[1-[(aminoiminomethyl)hydrazono]ethyl]phenyl]decanediamide
- Cni 1493
- Cni-1493
- CPSI 2364
- N,N'-bis[3-[(E)-N-(diaminomethylideneamino)-C-methylcarbonimidoyl]-5-[(Z)-N-(diaminomethylideneamino)-C-methylcarbonimidoyl]phenyl]decanediamide
- AXD-455
- Decanediamide, N1,N10-bis[3,5-bis[1-[2-(aminoiminomethyl)hydrazinylidene]ethyl]phenyl]-
- CAS:
- 352513-83-8
- MF:
- C34H52N18O2
- MW:
- 744.9
- Product Categories:
-
- Pharmaceutical
- Mol File:
- 352513-83-8.mol
Semapimod Chemical Properties
- Density
- 1.39
- pka
- 14.28±0.70(Predicted)
Semapimod Usage And Synthesis
Uses
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[1][2][3].
in vivo
Semapimod (5 mg/kg; i.p; daily for 2 weeks) ameliorates endothelial dysfunction in Obese Zucker (OZ) rats[1].
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].
| 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. |
| Animal Model: | C57Bl/6 mice (GL261 cells were orthotopically implanted)[4] |
| Dosage: | 6 mg/kg/day |
| Administration: | Intracranially for 1 week, delivered via an osmotic pump |
| Result: | Inhibited tumor cell invasion by more than 75%. |
IC 50
CD40; IL-1β; IL-6; p38 MAPK
References
[1] Nishimatsu H, et al. Blockade of endogenous proinflammatory cytokines ameliorates endothelial dysfunction in obese Zucker rats. Hypertens Res. 2008;31(4):737‐743. DOI:10.1291/hypres.31.737
[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. DOI:10.1053/j.gastro.2008.10.017
[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. DOI:10.4049/jimmunol.1502135
[4] Miller IS, et al. Semapimod sensitizes glioblastoma tumors to ionizing radiation by targeting microglia. PLoS One. 2014 May 9;9(5):e95885. DOI:10.1371/journal.pone.0095885
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