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I0157 Sigma

Ibudilast

≥99% (HPLC), solid

Synonym: 2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl] 1-propanone, 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine, KC-404

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cyclic Nucleotide Metabolism,
assay   ≥99% (HPLC)
form   solid
color   white
solubility   DMSO: soluble28 mg/mL
  H2O: soluble4.5 mg/mL
storage temp.   2-8°C
Gene Information   human ... PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144)

Description

Biochem/physiol Actions

Phosphodiesterase IV (PDE4) inhbitor. Inhibits platelet aggregation. Anti-asthma drug.

Features and Benefits

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®,1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

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LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

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Safety & Documentation

Safety Information

Symbol 
GHS07  GHS07
Signal word 
Warning
Hazard statements 
Precautionary statements 
Personal Protective Equipment 
Hazard Codes (Europe) 
Xn
Risk Statements (Europe) 
Safety Statements (Europe) 
26-36
WGK Germany 
3
RTECS 
UR0711200

Documents

Certificate of Analysis

Certificate of Origin

Protocols & Articles

Articles

Discover Bioactive Small Molecules for Cyclic Nucleotides

Transmission of an extracellular signal across the cell membrane is initiated by activation of many types of hormone and neurotransmitter receptors, such as G-protein coupled receptors (GPCRs), and c...
Keywords: Antivirals, Cancer, Cardiovascular, Cellular processes, Diabetes, Diseases, Hormones, Neurotransmitters

Peer-Reviewed Papers

References

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Ibudilast attenuates astrocyte apoptosis via cyclic GMP signaling pathway in an in vitro reperfusion model. Takuma, K., et al Br. J. Pharmacol. 133, 841-848, (2001)

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Ibudilast suppresses TNFα production by glial cells functioning mainly as type III phosphodiesteraze inhibitor in CNS. Suzumura, A., et al Brain Res. 837, 203-212 , (1999)

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Potentiation of ibudilast inhibition of platelet aggregation in the presence of endothelial cells. Rile, G., et al Thromb. Res. 102, 239-246, (2001)

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Ibudilast in relapsing-remitting multiple sclerosis: a neuroprotectant? Barkhof F, Hulst HE, Drulovic J, et al. Neurology 74(13), 1033-40, (2010)

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Ibudilast (AV-411). A new class therapeutic candidate for neuropathic pain and opioid withdrawal syndromes. Ledeboer A, Hutchinson MR, Watkins LR, et al. Expert Opin. Investig. Drugs 16(7), 935-50, (2007)

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Modulation of morphine-induced antinociception in acute and chronic opioid treatment by ibudilast. Lilius TO, Rauhala PV, Kambur O, et al. Anesthesiology 111(6), 1356-64, (2009)

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[Chronic subdural hematoma--recurrence and prevention]. Sakakibara F, Tsuzuki N, Uozumi Y, et al. Brain Nerve 63(1), 69-74, (2011)

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[Effect of ibudilast on apoptosis of airway eosinophil in asthmatic guinea pigs]. Xu S, Lü WH, and Zhang HQ Yao Xue Xue Bao 44(7), 737-40, (2009)

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[Nicergoline, ibudilast, ifenprodil tartrate]. Arii T and Katayama Y Nihon Rinsho. 64 Suppl 7, 602-5, (2006)

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Ibudilast: a non-selective PDE inhibitor with multiple actions on blood cells and the vascular wall. Kishi Y, Ohta S, Kasuya N, et al. Cardiovasc. Drug Rev. 19(3), 215-25, (2001)

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Adolescent morphine exposure affects long-term microglial function and later-life relapse liability in a model of addiction. Schwarz JM and Bilbo SD J. Neurosci. 33(3), 961-71, (2013)

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Allosteric inhibition of macrophage migration inhibitory factor revealed by ibudilast. Cho Y, Crichlow GV, Vermeire JJ, et al. Proc. Natl. Acad. Sci. U. S. A. 107(25), 11313-8, (2010)

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The antinociceptive effect of the asthma drug ibudilast in rat models of peripheral and central neuropathic pain. Hama AT, Broadhead A, Lorrain DS, et al. J. Neurotrauma 29(3), 600-10, (2012)

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Prevention of paclitaxel-induced peripheral neuropathy by lithium pretreatment. Mo M, Erdelyi I, Szigeti-Buck K, et al. FASEB J. 26(11), 4696-709, (2012)

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Elucidation of a Structural Basis for the Inhibitor-Driven, p62 (SQSTM1)-Dependent Intracellular Redistribution of cAMP Phosphodiesterase-4A4 (PDE4A4). Day, J.P., et al. J. Med. Chem. 54, 3331-3347, (2011)

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Ibudilast inhibits cerebral aneurysms by down-regulating inflammation-related molecules in the vascular wall of rats. Yagi K, Tada Y, Kitazato KT, et al. Neurosurgery 66(3), 551-9; discussion 559, (2010)

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Glial cell modulators attenuate methamphetamine self-administration in the rat. Snider SE, Hendrick ES, and Beardsley PM Eur. J. Pharmacol. 701(1-3), 124-30, (2013)

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The glial cell modulator and phosphodiesterase inhibitor, AV411 (ibudilast), attenuates prime- and stress-induced methamphetamine relapse. Beardsley PM, Shelton KL, Hendrick E, et al. Eur. J. Pharmacol. 637(1-3), 102-8, (2010)

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The glial cell modulators, ibudilast and its amino analog, AV1013, attenuate methamphetamine locomotor activity and its sensitization in mice. Snider SE, Vunck SA, van den Oord EJ, et al. Eur. J. Pharmacol. 679(1-3), 75-80, (2012)

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Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast. Allcock RW, Blakli H, Jiang Z, et al. Bioorg. Med. Chem. Lett. 21(11), 3307-12, (2011)

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Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells. Kiebala M and Maggirwar SB PLoS ONE 6(4), e18633, (2011)

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Inhibition of paclitaxel-induced decreases in calcium signaling. Benbow JH, Mann T, Keeler C, et al. J. Biol. Chem. 287(45), 37907-16, (2012)

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Ibudilast, a mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery. Yamazaki T, Anraku T, and Matsuzawa S Eur. J. Pharmacol. 650(2-3), 605-11, (2011)

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Ibudilast, a phosphodiesterase inhibitor with anti-inflammatory activity, protects against ischemic brain injury in rats. Lee JY, Cho E, Ko YE, et al. Brain Res. 1431, 97-106, (2012)

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Cross-species comparisons of the pharmacokinetics of ibudilast. Sanftner LM, Gibbons JA, Gross MI, et al. Xenobiotica 39(12), 964-77, (2009)

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Effects of topical application of ibudilast for seasonal allergic conjunctivitis in patients wearing soft contact lenses. Sakuma K, Toshida H, Honda R, et al. Eye Contact Lens 35(5), 251-4, (2009)

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Vasodilator effects of ibudilast on retinal blood vessels in anesthetized rats. Noguchi M, Mori A, Sakamoto K, et al. Biol. Pharm. Bull. 32(11), 1924-7, (2009)

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Determination of ibudilast in human serum by high-performance liquid chromatography for pharmacokinetic study. Yoon H, Cho HY, and Lee YB Biomed. Chromatogr. 24(3), 324-8, (2010)

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Ibudilast, a phosphodiesterase inhibitor, in combination with low-dose aspirin potently inhibits guinea pig carotid artery thrombosis without extending bleeding time and causing gastric mucosal injury. Matsuzawa S, Hoshina K, Sueyoshi S, et al. Arzneimittelforschung 62(12), 545-53, (2012)

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Primary neuroprotection: the Holy Grail of multiple sclerosis therapy. Fox RJ Neurology 74(13), 1018-9, (2010)

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Ibudilast: a review of its pharmacology, efficacy and safety in respiratory and neurological disease. Rolan P, Hutchinson M, and Johnson K Expert Opin. Pharmacother. 10(17), 2897-904, (2009)

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Merck 14,4879

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