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AdipoGen Life Sciences
Ibudilast
40
CHF
CHF 40.00
In stock
AG-CR1-3738-M01010 mgCHF 40.00
AG-CR1-3738-M05050 mgCHF 70.00
AG-CR1-3738-M250250 mgCHF 280.00
| Product Details | |
|---|---|
| Synonyms | AV-411; KC-404; MN166; BRN 0656579; 2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone |
| Product Type | Chemical |
| Properties | |
| Formula |
C14H18N2O |
| MW | 230.3 |
| CAS | 50847-11-5 |
| RTECS | UR0711200 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (20mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | ZJVFLBOZORBYFE-UHFFFAOYSA-N |
| Smiles | CC(C)C1=NN(C=CC=C2)C2=C1C(C(C)C)=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Ibudilast is a non-selective PDE (phosphodiesterase) inhibitor found to have anti-inflammatory activity primarily targeting the peripheral immune system and in the CNS via attenuation of glial cells.
- Ibudilast is an inhibitor of phosphodiesterase 4 (PDE4; IC50s = 54, 65, 239 and 166nM for PDE4A-D, respectively), PDE3A, PDE3B and PDE5A (IC50s = 1600, 2700 and 3510nM, respectively) and has been shown to act as a toll-like receptor 4 (TLR4) antagonist.
- Ibudilast is an allosteric inhibitor of macrophage inhibitory factor (MIF), which regulates the immune response known to drive inflammation and the cytokine storm. Overexpression of MIF is linked to multiple disease, including ARDS, asthma, rheumatoid arthritis, lupus and multiple sclerosis. Blocking the effects of MIF can protect patients with COVID-19 from developing ARDS.
- Ibudilast has bronchodilator, vasodilator (preventing the breakdown of secondary messengers cAMP and cGMP) and neuroprotective/anti-neuroinflammatory effects, is used in asthma and stroke treatment, inhibits platelet aggregation and may be usefull in certain brain disorders. It has been shown to be useful in the treatment of neuropathic pain and reducing methamphetamine, opioid and alcohol addiction. It also has antiviral properties, inhibiting replication of HIV-1.
Product References
- KC-404: a potential anti-allergic agent with antagonistic action against slow reacting substance of anaphylaxis: K. Nishino, et al.; Jpn. J. Pharmacol. 33, 267 (1983)
- Pharmacological studies on newly synthesized anti-allergic agents, 2-methyl-3-piperidino-beta-propionaphtone hydrochloride (KZ-111) and 3-isobutyryl-2-isopropylpyrazole-[1, 5-a] pyridine (KC-404): H. Nagai, et al.; Jpn. J. Pharmacol. 33, 1215 (1983)
- Effect of ibudilast: a novel antiasthmatic agent, on airway hypersensitivity in bronchial asthma: A. Kawasaki, et al.; J. Asthma. 29, 245 (1992)
- Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia: T. Mizuno, et al.; Neuropharmacol. 46, 404 (2004)
- Preferential inhibition of human phosphodiesterase 4 by ibudilast: Z. Huang, et al.; Life Sci. 78, 2663 (2006)
- The inhibitory profile of Ibudilast against the human phosphodiesterase enzyme family: L.C. Gibson, et al.; Eur. J. Pharmacol. 538, 39 (2006)
- Ibudilast (AV-411). A new class therapeutic candidate for neuropathic pain and opioid withdrawal syndromes: A. Ledeboer, et al.; Expert Opin. Investig. Drugs 16, 935 (2007)
- Allosteric inhibition of macrophage migration inhibitory factor revealed by ibudilast: Y. Cho, et al.; PNAS 107, 11313 (2010)
- Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells: M. Kiebala & S.B. Maggirwar; PLoS One 6, e18633 (2011)
- Ibudilast, a phosphodiesterase inhibitor with anti-inflammatory activity, protects against ischemic brain injury in rats: J.Y. Lee, et al.; Brain Res. 1431, 97 (2012)
- Ibudilast reduces alcohol drinking in multiple animal models of alcohol dependence: R.L. Bell, et al.; Addict. Biol. 20, 38 (2015)
- Ibudilast (AV411), and its AV1013 analog, reduce HIV-1 replication and neuronal death induced by HIV-1 and morphine: N. El-Hage, et al.; AIDS 28, 1409 (2014)
- The effects of ibudilast, a glial activation inhibitor, on opioid withdrawal symptoms in opioid-dependent volunteers: Z.D. Cooper, et al.; Addict. Biol. 21, 895 (2016)
- The Effects of the Toll-Like Receptor 4 Antagonist, Ibudilast, on Sevoflurane's Minimum Alveolar Concentration and the Delayed Remifentanil-Induced Increase in the Minimum Alveolar Concentration in Rats: D. Ruiz-Perez, et al.; Anesth. Analg. 122, 1370 (2016)
- Ibudilast for the treatment of multiple sclerosis: A.D. Goodman, et al.; Expert Opin. Investig. Drugs 25, 1231 (2016)
- Ibudilast, a Phosphodiesterase-4 Inhibitor, Ameliorates Acute Respiratory Distress Syndrome in Neonatal Mice by Alleviating Inflammation and Apoptosis: D. Yang, et al.; Med. Sci. Monit. 26, e922281 (2020)
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