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HomeProduct name listIbudilast

Ibudilast

Synonym(s):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

  • CAS NO.:50847-11-5
  • Empirical Formula: C14H18N2O
  • Molecular Weight: 230.31
  • MDL number: MFCD00864808
  • EINECS: 637-150-7
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-01 14:32:37
Ibudilast Structural

What is Ibudilast?

Description

Ibudilast is a leukomene antagonist and phosphodiesterase inhibitor useful in the treatment of bronchial asthma. It antagonizes leukotriene D4-induced contractions of guinea pig ileum and tracheal muscles in virro, and inhibits eosinophil accumulation in vivo.

Chemical properties

White Solid

Originator

Kyorin (Japan)

The Uses of Ibudilast

Inhibitors of phosphodiesterase 4 (PDE4), which catalyzes the hydrolysis of cAMP, have potential applications in a variety of diseases, including asthma. Ibudilast is an inhibitor of PDE4 (IC50 = 54-239 nM) that, at higher doses, also inhibits PDE3 and PDE5 (IC50 = 1,600-3,510 nM). Through this action, it suppresses the elaboration of mediators involved in asthma and inflammation.[Cayman Chemical]

The Uses of Ibudilast

A leukotriene D4 antagonist. Used as an antiallergic, antiasthmatic, and vasodilator (cerebral)

The Uses of Ibudilast

a phosphodiesterase inhibitor with anti-inflammatory activity

What are the applications of Application

Ibudilast is a nonselective phosphodiesterase inhibitor

Definition

ChEBI: Ibudilast is a pyrazolopyridine.

brand name

Ketas

Biological Activity

Phosphodiesterase inhibitor (IC 50 values are 53, 35, 48, 12 and 10 mM for PDE Ia, II, III, IV and V respectively). Inhibits platelet aggregation and is an orally-active cerebral vasodilator, bronchodilator and antiallergic agent.

Biochem/physiol Actions

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

in vitro

ibudilast could potently inhibit purified human pde4a, 4b, 4c and 4d with ic50 values at 54, 65, 239 and 166 nm, respectively. ibudilast was also able to effectively block lps-induced tumor necrosis factor and n-formyl-metleu-phe-induced leukotriene b4 biosynthesis in human whole blood [1].

in vivo

rats received a daily oral administration of 10, 30 or 60 mg/kg ibudilast. results showed that in the vehicle-treated animals, white matter lesions and microglial activation occurred in the optic tract, internal capsule and corpus callosum. a low dose of ibudilast failed to suppress the white matter lesions and microglial activation, whereas a dose of either 30 or 60 mg/kg ibudilast ameliorated these lesions [2].

storage

Store at RT

References

1) Kishi et al. (2001), Ibudilast: a non-selective PDE inhibitor with multiple actions on blood cells and the vascular wall; Cardiovasc. Drug Rev., 19 215 2) Yamazaki et al. (2011), Ibudilast. A mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery; Eur. J. Pharmacol., 650 605 3) Cueva Vargas et al. (2016), The glial cell modulator ibudilast attenuates neuroinflammation and enhances retinal ganglion cell viability in glaucoma through protein kinase A signaling.; Neurobiol. Dis., 93 156 4) Mizuno et al. (2004), Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia; Neuropharmacology, 46 404 5) Ledeboer et al. (2007), Ibudilast (AV-411). A class therapeutic candidate for neuropathic pain and opioid withdrawal syndromes; Expert. Opin. Investig. Drugs, 16 935

Properties of Ibudilast

Melting point: 53-54°C
Boiling point: 175°C/7.5mmHg(lit.)
Density  1.09
refractive index  1.5500 (estimate)
storage temp.  Sealed in dry,2-8°C
solubility  DMSO: 28 mg/mL, soluble
form  solid
pka 1.22±0.30(Predicted)
color  white
Merck  14,4879
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
CAS DataBase Reference 50847-11-5(CAS DataBase Reference)

Safety information for Ibudilast

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P270:Do not eat, drink or smoke when using this product.
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for Ibudilast

InChIKey ZJVFLBOZORBYFE-UHFFFAOYSA-N

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