Ibudilast
Product Code: AG-CR1-3738
Product Group: Natural Products and Extracts
Supplier: AdipoGen Life Sciences
| Code | Size | Price |
|---|
| AG-CR1-3738-M010 | 10 mg | £40.00 |
Quantity:
| AG-CR1-3738-M050 | 50 mg | £70.00 |
Quantity:
| AG-CR1-3738-M250 | 250 mg | £250.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Documents
Further Information
Alternate Names/Synonyms:
AV-411; KC-404; MN166; BRN 0656579; 2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone
Appearance:
White to off-white solid.
CAS:
50847-11-5
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Keep cool and dry.
Hazards:
H302, H315, H317, H319, H335
InChi:
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
InChiKey:
ZJVFLBOZORBYFE-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 50847-11-5. Formula: C14H18N2O. MW: 230.3. 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.
MDL:
MFCD00864808
Molecular Formula:
C14H18N2O
Molecular Weight:
230.3
Package Type:
Vial
Precautions:
P301+P312, P302+P352, P304+P340, P305+P351+P338
Product 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.
Purity:
>98% (HPLC)
Signal word:
Warning
SMILES:
CC(C)C1=NN(C=CC=C2)C2=C1C(C(C)C)=O
Solubility Chemicals:
Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (20mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Natural Products/Extracts
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)