1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

Ibudilast (Synonyms: KC-404; AV-411; MN-166)

Cat. No.: HY-B0763 Purity: 99.83%
Data Sheet SDS Handling Instructions

Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor which has been marketed for treating asthma.

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Ibudilast Chemical Structure

Ibudilast Chemical Structure

CAS No. : 50847-11-5

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10 mM * 1 mL in DMSO $85 In-stock
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Description

Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor which has been marketed for treating asthma. Target: PDE Ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE). The inhibition of platelet aggregation and vasodilatation by ibudilast may be due to synergistic elevation of intracellular cyclic nucleotides and release of nitric oxide (NO) or prostacyclin from endothelium, rather than direct inhibition of PDE5 or PDE3. Another important property of ibudilast is its antiinflammatory activity possibly associated with potent inhibition of PDE4. Combined with its relaxing effects on bronchial smooth muscle, antiinflammatory actvity of ibudilast could favorably influence pathophysiology of asthma by antagonizing chemical mediators triggering asthmatic attacks [1, 2]. Ibudilast (AV-411) is a non-selective phosphodiesterase inhibitor that is also known to suppress glial cell activation. Preclinical data indicate that ibudilast crosses the blood-brain barrier, is well tolerated, is active on oral administration, reduces glial activation and attenuates pain symptoms in diverse rat models of neuropathic pain. In addition, it enhances acute morphine analgesia and attenuates morphine tolerance and withdrawal. Thus ibudilast may improve opioid efficacy and is a promising therapeutic candidate for neuropathic pain, with a novel mechanism of action [3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02714036 MediciNova|Massachusetts General Hospital|South Shore Neurologic Associates Amyotrophic Lateral Sclerosis March 2016 Phase 1|Phase 2
NCT02025998 University of California, Los Angeles|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Alcohol Use Disorders December 2013 Phase 1
NCT01389193 Parisa Gazerani|The Ministry of Science, Technology and Innovation, Denmark|Migraine Research Foundation|Aalborg University Migraine Headache June 2013 Phase 1
NCT01317992 University of Adelaide|University of South Australia Medication Overuse Headache April 2011 Phase 1|Phase 2
NCT01217970 University of California, Los Angeles|National Institute on Drug Abuse (NIDA)|MediciNova Methamphetamine-dependence|Substance Abuse January 2011 Phase 1
NCT01860807 University of California, Los Angeles|National Institute on Drug Abuse (NIDA) Methamphetamine Dependence|HIV Infection July 2013 Phase 2
NCT01982942 MediciNova|National Institutes of Health (NIH)|National Institute of Neurological Disorders and Stroke (NINDS)|National Multiple Sclerosis Society Multiple Sclerosis, Primary Progressive|Multiple Sclerosis, Secondary Progressive November 2013 Phase 2
NCT02238626 MediciNova|Carolinas Healthcare System Amyotrophic Lateral Sclerosis September 2014 Phase 2
NCT01740414 New York State Psychiatric Institute|National Institute on Drug Abuse (NIDA)|MediciNova Opioid Abuse|Opioid Dependence November 2012 Phase 2
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References
Molecular Weight

230.31

Formula

C₁₄H₁₈N₂O

CAS No.

50847-11-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Ibudilast
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