Apilimod mesylate

This product is for research use only, not for human use. We do not sell to patients.

Apilimod mesylate
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
500mg$480Check With Us
1g$780Check With Us
1g$1170Check With Us

Cat #: V4143 CAS #: 870087-36-8 Purity ≥ 98%

Description: Apilimod mesylate, the mesylate salt of Apilimod, is a novel and potent small molecular inhibitor of IL-12/IL-23 and has been evaluated in clinical trials for patients with Crohn's disease or rheumatoid arthritis.

References: Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64.

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Molecular Weight (MW)610.70
Molecular FormulaC25H34N6O8S2
CAS No.870087-36-8
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeCC1=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=NC=CC=C4)=N2)=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O
SynonymsSTA-5326; STA5326; STA 5326; LAM-002; LAM 002; LAM002; Apilimod; Apilimod mesylate
ProtocolIn VitroApilimod inhibits IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod.
In VivoApilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. Apilimod causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.6375 mL8.1873 mL16.3747 mL32.7493 mL
5mM0.3275 mL1.6375 mL3.2749 mL6.5499 mL
10mM0.1637 mL0.8187 mL1.6375 mL3.2749 mL
20mM0.0819 mL0.4094 mL0.8187 mL1.6375 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
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.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.