Ibudilast

Bezeichnung:Ibudilast

CAS-Nr50847-11-5

Englisch Name:Ibudilast

CBNumberCB0145945

SummenformelC14H18N2O

Molgewicht230.31

MOL-Datei50847-11-5.mol

Ibudilast physikalisch-chemischer Eigenschaften

Schmelzpunkt	53-54°C
Siedepunkt	175°C/7.5mmHg(lit.)
Dichte	1.09
Brechungsindex	1.5500 (estimate)
storage temp.	Sealed in dry,2-8°C
Löslichkeit	DMSO: 28 mg/mL, soluble
Aggregatzustand	solid
pka	1.22±0.30(Predicted)
Farbe	white
Merck	14,4879
Stabilität	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.
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
SMILES	C(C1=C2N(N=C1C(C)C)C=CC=C2)(=O)C(C)C
CAS Datenbank	50847-11-5(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36/37/38
S-Sätze:	26-36
WGK Germany	3
RTECS-Nr.	UR0711200
HS Code	2933.99.8290
Toxizität	LD50 i.v. in mice: 260 mg/kg (Irikura, 1973)

Gefahreninformationscode (GHS)

Ibudilast Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.
Chemische Eigenschaften
White Solid
Originator
Kyorin (Japan)
Verwenden
a phosphodiesterase inhibitor with anti-inflammatory activity
Verwenden
A leukotriene D4 antagonist. Used as an antiallergic, antiasthmatic, and vasodilator (cerebral)
Verwenden
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]
Definition
ChEBI: Ibudilast is a pyrazolopyridine.
Trademarks
Ketas
Biologische Aktivität
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].
IC 50
54-239 nm
Lager
Store at RT
Einzelnachweise
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

Ibudilast Upstream-Materialien And Downstream Produkte

Ibudilast Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

50847-11-5, Ibudilast Verwandte Suche:

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