Apilimod mesylate

Synonyms: STA-5326 mesylate

Apilimod mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod mesylate (STA-5326 mesylate) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.

Apilimod mesylate Chemical Structure

Apilimod mesylate Chemical Structure

CAS: 870087-36-8

Selleck's Apilimod mesylate has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.87%
99.87

Choose Selective Interleukins Inhibitors

Biological Activity

Description Apilimod mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod mesylate (STA-5326 mesylate) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
Targets
IL-12 [1]
(in IFN-γ/SAC-stimulated human PBMCs)
IL-12 [1]
(in human monocytes)
IL-12 [1]
(in mouse PBMCs)
PIKfyve [2]
(Cell-free assay)
1 nM 1 nM 2 nM 14 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00234741 Completed Crohn''s Disease Synta Pharmaceuticals Corp.|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) November 2005 Phase 2

Chemical lnformation & Solubility

Molecular Weight 610.7 Formula

C25H34N6O8S2

CAS No. 870087-36-8 SDF --
Smiles CC1=CC(=CC=C1)C=NNC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4.CS(=O)(=O)O.CS(=O)(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 33 mg/mL

DMSO : 20 mg/mL ( (32.74 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Apilimod mesylate | Apilimod mesylate supplier | purchase Apilimod mesylate | Apilimod mesylate cost | Apilimod mesylate manufacturer | order Apilimod mesylate | Apilimod mesylate distributor