1. Apoptosis Immunology/Inflammation MAPK/ERK Pathway
  2. TNF Receptor Interleukin Related p38 MAPK
  3. Semapimod tetrahydrochloride

Semapimod tetrahydrochloride  (Synonyms: CNI-1493; CPSI-2364 tetrahydrochloride)

Cat. No.: HY-15509A Purity: 98.43%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Semapimod tetrahydrochloride Chemical Structure

Semapimod tetrahydrochloride Chemical Structure

CAS No. : 164301-51-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Semapimod tetrahydrochloride:

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1 Publications Citing Use of MCE Semapimod tetrahydrochloride

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  • Biological Activity

  • Purity & Documentation

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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].

IC50 & Target[1][2][3]

IL-1β

 

IL-6

 

p38 MAPK

 

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].
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 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].
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.

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%.
Clinical Trial
Molecular Weight

890.74

Formula

C34H56Cl4N18O2

CAS No.
Appearance

Solid

Color

White to yellow

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.Cl.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

H2O : 2.17 mg/mL (2.44 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1227 mL 5.6133 mL 11.2266 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Working solution concentration: mg/mL
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.43%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.1227 mL 5.6133 mL 11.2266 mL 28.0666 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Semapimod tetrahydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Semapimod tetrahydrochloride
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