Ibudilast
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319626

CAS#: 50847-11-5

Description: Ibudilast, also known as AV-411, KC-404 and MN-166, is an antiinflammatory drug used mainly in Japan, which acts as a phosphodiesterase inhibitor, inhibiting the PDE-4 subtype to the greatest extent, but also showing significant inhibition of other PDE subtypes. Ibudilast has bronchodilator, vasodilator and neuroprotective effects, and is mainly used in the treatment of asthma and stroke. It inhibits platelet aggregation, and may also be useful in the treatment of multiple sclerosis.

Chemical Structure

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Ibudilast
CAS# 50847-11-5
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319626
Name: Ibudilast
CAS#: 50847-11-5
Chemical Formula: C14H18N2O
Exact Mass: 230.14
Molecular Weight: 230.311
Elemental Analysis: C, 73.01; H, 7.88; N, 12.16; O, 6.95

Price and Availability

Size Price Availability Quantity
25mg USD 350
50mg USD 650
100mg USD 1150
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Synonym: MN-166, MN166, MN 166, AV-411, AV 411, AV411, KC404; KC-404; KC 404; Ibudilast

IUPAC/Chemical Name: 2-methyl-1-(2-propan-2-ylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one

InChi Key: ZJVFLBOZORBYFE-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3

SMILES Code: CC(C)C(C1=C2C=CC=CN2N=C1C(C)C)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Certificate of Analysis:
View CoA: current batch, Lot#C9M05C09
Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)
Instruction:
View handling instruction
Biological target: Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects.
In vitro activity: Ibudilast suppressed the increase in MUC5AC released from the cells treated with any concentration of TGF-α; this effect was observed even at the highest concentration (100 ng/mL) (Fig. 1B). Reference: Biol Pharm Bull. 2021;44(3):404-409. https://pubmed.ncbi.nlm.nih.gov/33642548/
In vivo activity: This study observed that IBD (ibudilast) ameliorated this reduction in temperature (Fig. 1A). Administration of LPS upregulated IL-6 levels, whereas IBD reduced the upregulated IL-6 levels (Fig. 1B). Reference: Biol Pharm Bull. 2022;45(8):1180-1184. https://pubmed.ncbi.nlm.nih.gov/35908899/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 20.0 86.84
DMSO 56.3 244.27
Ethanol 31.3 136.09
Ethanol:PBS (pH 7.2) (1:11) 0.1 0.35
Water 30.0 130.26

Preparing Stock Solutions

The following data is based on the product molecular weight 230.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Ishibashi J, Saito K, Ishizaki T, Horie I, Isohama Y. Ibudilast Suppresses MUC5AC Mucus Production through Inhibition of ERK1/2 Phosphorylation. Biol Pharm Bull. 2021;44(3):404-409. doi: 10.1248/bpb.b20-00798. PMID: 33642548. 2. Chang Y, Hu CC, Wu YY, Ueng SWN, Chang CH, Chen MF. Ibudilast Mitigates Delayed Bone Healing Caused by Lipopolysaccharide by Altering Osteoblast and Osteoclast Activity. Int J Mol Sci. 2021 Jan 25;22(3):1169. doi: 10.3390/ijms22031169. PMID: 33503906; PMCID: PMC7865869. 3. Kadota N, Yoshida A, Sawamoto A, Okuyama S, Nakajima M. Ibudilast Reduces IL-6 Levels and Ameliorates Symptoms in Lipopolysaccharide-Induced Sepsis Mice. Biol Pharm Bull. 2022;45(8):1180-1184. doi: 10.1248/bpb.b22-00284. PMID: 35908899. 4. Egashira N, Goto Y, Takahashi R, Iba H, Yamamoto S, Watanabe T, Kubota K, Kawashiri T, Taniguchi C, Katsurabayashi S, Iwasaki K. Ibudilast suppresses oxaliplatin-induced mechanical allodynia and neurodegeneration in rats. J Pharmacol Sci. 2021 Sep;147(1):114-117. doi: 10.1016/j.jphs.2021.06.004. Epub 2021 Jun 12. PMID: 34294361.
In vitro protocol: 1. Ishibashi J, Saito K, Ishizaki T, Horie I, Isohama Y. Ibudilast Suppresses MUC5AC Mucus Production through Inhibition of ERK1/2 Phosphorylation. Biol Pharm Bull. 2021;44(3):404-409. doi: 10.1248/bpb.b20-00798. PMID: 33642548. 2. Chang Y, Hu CC, Wu YY, Ueng SWN, Chang CH, Chen MF. Ibudilast Mitigates Delayed Bone Healing Caused by Lipopolysaccharide by Altering Osteoblast and Osteoclast Activity. Int J Mol Sci. 2021 Jan 25;22(3):1169. doi: 10.3390/ijms22031169. PMID: 33503906; PMCID: PMC7865869.
In vivo protocol: 1. Kadota N, Yoshida A, Sawamoto A, Okuyama S, Nakajima M. Ibudilast Reduces IL-6 Levels and Ameliorates Symptoms in Lipopolysaccharide-Induced Sepsis Mice. Biol Pharm Bull. 2022;45(8):1180-1184. doi: 10.1248/bpb.b22-00284. PMID: 35908899. 2. Egashira N, Goto Y, Takahashi R, Iba H, Yamamoto S, Watanabe T, Kubota K, Kawashiri T, Taniguchi C, Katsurabayashi S, Iwasaki K. Ibudilast suppresses oxaliplatin-induced mechanical allodynia and neurodegeneration in rats. J Pharmacol Sci. 2021 Sep;147(1):114-117. doi: 10.1016/j.jphs.2021.06.004. Epub 2021 Jun 12. PMID: 34294361.

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1: Johnson JL, Kwok YH, Sumracki NM, Swift JE, Hutchinson MR, Johnson K, Williams DB, Tuke J, Rolan PE. Glial Attenuation With Ibudilast in the Treatment of Medication Overuse Headache: A Double-Blind, Randomized, Placebo-Controlled Pilot Trial of Efficacy and Safety. Headache. 2015 Oct;55(9):1192-208. doi: 10.1111/head.12655. Epub 2015 Sep 14. PubMed PMID: 26367865.

2: Cooper ZD, Johnson KW, Pavlicova M, Glass A, Vosburg SK, Sullivan MA, Manubay JM, Martinez DM, Jones JD, Saccone PA, Comer SD. The effects of ibudilast, a glial activation inhibitor, on opioid withdrawal symptoms in opioid-dependent volunteers. Addict Biol. 2015 May 14. doi: 10.1111/adb.12261. [Epub ahead of print] PubMed PMID: 25975386; PubMed Central PMCID: PMC4644513.

3: Charntikov S, Pittenger ST, Thapa I, Bastola DR, Bevins RA, Pendyala G. Ibudilast reverses the decrease in the synaptic signaling protein phosphatidylethanolamine-binding protein 1 (PEBP1) produced by chronic methamphetamine intake in rats. Drug Alcohol Depend. 2015 Jul 1;152:15-23. doi: 10.1016/j.drugalcdep.2015.04.012. Epub 2015 Apr 30. PubMed PMID: 25962787.

4: Wang H, Mei Zl, Zhong KL, Hu M, Long Y, Miao MX, Li N, Yan TH, Hong H. Pretreatment with antiasthmatic drug ibudilast ameliorates Aβ 1-42-induced memory impairment and neurotoxicity in mice. Pharmacol Biochem Behav. 2014 Sep;124:373-9. doi: 10.1016/j.pbb.2014.07.006. Epub 2014 Jul 17. PubMed PMID: 25038445.

5: El-Hage N, Rodriguez M, Podhaizer EM, Zou S, Dever SM, Snider SE, Knapp PE, Beardsley PM, Hauser KF. Ibudilast (AV411), and its AV1013 analog, reduce HIV-1 replication and neuronal death induced by HIV-1 and morphine. AIDS. 2014 Jun 19;28(10):1409-19. doi: 10.1097/QAD.0000000000000291. PubMed PMID: 24732776; PubMed Central PMCID: PMC4300098.

6: Ellis A, Wieseler J, Favret J, Johnson KW, Rice KC, Maier SF, Falci S, Watkins LR. Systemic administration of propentofylline, ibudilast, and (+)-naltrexone each reverses mechanical allodynia in a novel rat model of central neuropathic pain. J Pain. 2014 Apr;15(4):407-21. doi: 10.1016/j.jpain.2013.12.007. Epub 2014 Jan 9. PubMed PMID: 24412802; PubMed Central PMCID: PMC3972272.

7: Bell RL, Lopez MF, Cui C, Egli M, Johnson KW, Franklin KM, Becker HC. Ibudilast reduces alcohol drinking in multiple animal models of alcohol dependence. Addict Biol. 2015 Jan;20(1):38-42. doi: 10.1111/adb.12106. Epub 2013 Nov 11. PubMed PMID: 24215262; PubMed Central PMCID: PMC4017009.

8: Zhaleh M, Panahi M, Ghafurian Broujerdnia M, Ghorbani R, Ahmadi Angali K, Saki G. Role of phosphodiesterase inhibitor Ibudilast in morphine-induced hippocampal injury. J Inj Violence Res. 2014 Jul;6(2):72-8. doi: 10.5249/jivr.v6i2.497. Epub 2013 Oct 11. PubMed PMID: 24121451; PubMed Central PMCID: PMC4009172.

9: Inoue N, Fukuda S, Inada T, Sameshima E, Tokushima Y, Harada M. Effect of ibudilast on the reciprocal inhibitory visual-vestibular interaction closely related to dizziness after cerebral ischemia. J Stroke Cerebrovasc Dis. 2014 Jan;23(1):51-5. doi: 10.1016/j.jstrokecerebrovasdis.2012.09.007. Epub 2012 Oct 22. PubMed PMID: 23085301.

10: Matsuzawa S, Hoshina K, Sueyoshi S, Miyata Y, Manita S, Ooie T, Yasue T, Sasahara T. 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. Arzneimittelforschung. 2012 Dec;62(12):545-53. doi: 10.1055/s-0032-1323699. Epub 2012 Sep 3. PubMed PMID: 22945770.

11: Snider SE, Vunck SA, van den Oord EJ, Adkins DE, McClay JL, Beardsley PM. The glial cell modulators, ibudilast and its amino analog, AV1013, attenuate methamphetamine locomotor activity and its sensitization in mice. Eur J Pharmacol. 2012 Mar 15;679(1-3):75-80. doi: 10.1016/j.ejphar.2012.01.013. Epub 2012 Jan 28. PubMed PMID: 22306241; PubMed Central PMCID: PMC3973724.

12: Lee JY, Cho E, Ko YE, Kim I, Lee KJ, Kwon SU, Kang DW, Kim JS. Ibudilast, a phosphodiesterase inhibitor with anti-inflammatory activity, protects against ischemic brain injury in rats. Brain Res. 2012 Jan 11;1431:97-106. doi: 10.1016/j.brainres.2011.11.007. Epub 2011 Nov 9. PubMed PMID: 22137656.

13: Hama AT, Broadhead A, Lorrain DS, Sagen J. The antinociceptive effect of the asthma drug ibudilast in rat models of peripheral and central neuropathic pain. J Neurotrauma. 2012 Feb 10;29(3):600-10. doi: 10.1089/neu.2011.1863. Epub 2011 Oct 19. PubMed PMID: 21806469.

14: Allcock RW, Blakli H, Jiang Z, Johnston KA, Morgan KM, Rosair GM, Iwase K, Kohno Y, Adams DR. Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3307-12. doi: 10.1016/j.bmcl.2011.04.021. Epub 2011 Apr 13. PubMed PMID: 21530250.

15: Kiebala M, Maggirwar SB. Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells. PLoS One. 2011 Apr 8;6(4):e18633. doi: 10.1371/journal.pone.0018633. PubMed PMID: 21494611; PubMed Central PMCID: PMC3072977.

16: Yamazaki T, Anraku T, Matsuzawa S. Ibudilast, a mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery. Eur J Pharmacol. 2011 Jan 15;650(2-3):605-11. doi: 10.1016/j.ejphar.2010.10.033. Epub 2010 Oct 29. PubMed PMID: 21036126.

17: Cho Y, Crichlow GV, Vermeire JJ, Leng L, Du X, Hodsdon ME, Bucala R, Cappello M, Gross M, Gaeta F, Johnson K, Lolis EJ. Allosteric inhibition of macrophage migration inhibitory factor revealed by ibudilast. Proc Natl Acad Sci U S A. 2010 Jun 22;107(25):11313-8. doi: 10.1073/pnas.1002716107. Epub 2010 Jun 8. PubMed PMID: 20534506; PubMed Central PMCID: PMC2895110.

18: Beardsley PM, Shelton KL, Hendrick E, Johnson KW. The glial cell modulator and phosphodiesterase inhibitor, AV411 (ibudilast), attenuates prime- and stress-induced methamphetamine relapse. Eur J Pharmacol. 2010 Jul 10;637(1-3):102-8. doi: 10.1016/j.ejphar.2010.04.010. Epub 2010 Apr 23. PubMed PMID: 20399770; PubMed Central PMCID: PMC2878837.

19: Barkhof F, Hulst HE, Drulovic J, Uitdehaag BM, Matsuda K, Landin R; MN166-001 Investigators. Ibudilast in relapsing-remitting multiple sclerosis: a neuroprotectant? Neurology. 2010 Mar 30;74(13):1033-40. doi: 10.1212/WNL.0b013e3181d7d651. Epub 2010 Mar 3. PubMed PMID: 20200338.

20: Yagi K, Tada Y, Kitazato KT, Tamura T, Satomi J, Nagahiro S. Ibudilast inhibits cerebral aneurysms by down-regulating inflammation-related molecules in the vascular wall of rats. Neurosurgery. 2010 Mar;66(3):551-9; discussion 559. doi: 10.1227/01.NEU.0000365771.89576.77. PubMed PMID: 20124930.