Name: Ibudilast
Brand: Selleck Chemicals
SKU: S4837
Availability: InStock
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PDE Products	Rolipram IBMX (3-Isobutyl-1-methylxanthine) Icariin Mardepodect (PF-2545920) Cilomilast Deltarasin PF-8380 Enpp-1-IN-1 GSK256066 Ziritaxestat (GLPG1690)

Solubility

In vitro
Batch:

DMSO : 46 mg/mL (199.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (17.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (17.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	230.31	Formula	C₁₄H₁₈N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	50847-11-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	KC-404, AV411, MN166			Smiles	CC(C)C1=NN2C=CC=CC2=C1C(=O)C(C)C

Mechanism of Action

Targets/IC₅₀/Ki	PDE4 (Bovine aortic EC) 0.08 μM PDE2 (Bovine aortic EC) 0.11 μM PDE5 (Human platelets) 2.2 μM
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).
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, this compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11607039/ [2] https://pubmed.ncbi.nlm.nih.gov/8650721/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Ibudilast PDE inhibitor

Chemical Structure

Molecular Weight: 230.31