Home Metabolism PDE inhibitor Ibudilast For research use only.

Ibudilast

Synonyms: KC-404, AV411, MN166

Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.

Ibudilast Chemical Structure

Ibudilast Chemical Structure

CAS No. 50847-11-5

Purity & Quality Control

Ibudilast Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

Biological Activity

Description Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
Targets
PDE4 [1]
(Bovine aortic EC)		 PDE2 [1]
(Bovine aortic EC)		 PDE5 [1]
(Human platelets)
0.08 μM 0.11 μM 2.2 μM
In vitro
In vitro Ibudilast suppressses pro-inflammatory cytokines (IL-6, IL-1β, TNF-α), toll-like receptor 4 blockade (TLR-4); inhibits a macrophage migration inhibitory factor (MIF), upregulates the anti‑inflammatory cytokine (IL-10) and promotes neurotrophic factors (GDNF, NGF, NT‑4)[1].
In Vivo
In vivo Ibudilast crosses the blood-brain barrier and has a good tolerance in vivo. It inhibits platelet aggregation, improves cerebral blood flow and attenuates allergic reactions in clinical applications. In an animal model of encephalomyelitis, Ibudilast significantly attenuates inflammatory cell infiltration in the lumbar spinal cord. After oral administration, it is well absorbed and metabolized in the liver mainly to diOH-ibudilast, which has similar or even stronger pharmacological effects[1].
Animal Research Animal Models A gerbil model of carotid artery thrombosis
Dosages 0.3 and 1.0 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04054206 Completed
Healthy Volunteers
MediciNova
 June 24 2019 Phase 1
NCT03341078 Recruiting
Methamphetamine-dependence
VA Office of Research and Development|Portland VA Medical Center|Oregon Health and Science University
 May 1 2019 Phase 2
NCT03782415 Active not recruiting
Glioblastoma|Recurrent Glioblastoma|GBM|Newly Diagnosed Glioblastoma
MediciNova
 December 29 2018 Phase 1|Phase 2
NCT02714036 Completed
Amyotrophic Lateral Sclerosis
MediciNova|Massachusetts General Hospital|South Shore Neurologic Associates
 May 6 2016 Phase 1|Phase 2
NCT00723177 Completed
Opioid-Related Disorders
New York State Psychiatric Institute|National Institute on Drug Abuse (NIDA)
 October 2008 Phase 2
NCT00576277 Completed
Diabetic Neuropathy
Avigen
 September 2006 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 230.31 Formula

C14H18N2O
CAS No. 50847-11-5 SDF --
Smiles CC(C)C1=NN2C=CC=CC2=C1C(=O)C(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (199.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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

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