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Semapimod tetrahydrochloride

Names

[ CAS No. ]:
164301-51-3

[ Name ]:
Semapimod tetrahydrochloride

[Synonym ]:
Semapimod HCl
Decanediamide,N,N'-bis(3,5-bis(1-((aminoiminomethyl)hydrazono)ethyl)phenyl)-,tetrahydrochloride
CNI 1493
AXD 455
N,N'-Bis(3,5-bis(1-((aminoiminomethyl)hydrazono)ethyl)phenyl)decanediamide tetrahydrochloride
Semapimod tetrahydrochloride
Semapimod hydrochloride

Biological Activity

[Description]:

Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈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[1][2][3].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Inflammation/Immunology

[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[2]. 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[3].

[In Vivo]

Semapimod tetrahydrochloride (5 mg/kg; i.p; daily for 2 weeks) ameliorates endothelial dysfunction in Obese Zucker (OZ) rats[1]. Semapimod tetrahydrochloride restores AM-induced akt phosphorylation and cGMP production in OZ rats[1]. 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.

[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.

[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.

[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.

Chemical & Physical Properties

[ Boiling Point ]:
1025.8ºC at 760mmHg

[ Molecular Formula ]:
C34H56Cl4N18O2

[ Molecular Weight ]:
890.74000

[ Flash Point ]:
574.2ºC

[ Exact Mass ]:
888.35900

[ PSA ]:
362.22000

[ LogP ]:
11.48360

[ Vapour Pressure ]:
0mmHg at 25°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds