Seratrodast

Bezeichnung:Seratrodast

CAS-Nr112665-43-7

Englisch Name:Seratrodast

CBNumberCB8284400

SummenformelC22H26O4

Molgewicht354.44

MOL-Datei112665-43-7.mol

Seratrodast physikalisch-chemischer Eigenschaften

Schmelzpunkt	118-120°C
Siedepunkt	522.3±49.0 °C(Predicted)
Dichte	1.140±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Chloroform (Slightly), Methanol (Slightly)
pka	4.76±0.10(Predicted)
Aggregatzustand	Yellow-orange solid.
Farbe	Pale Orange to Yellow
Merck	14,8459
CAS Datenbank	112665-43-7(CAS DataBase Reference)

Sicherheit

RTECS-Nr.	DA1600050
HS Code	2918.30.3000

Gefahreninformationscode (GHS)

Seratrodast Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Seratrodast, a novel benzoquinone derivative, is the first thromboxane A₂ (TxA₂) receptor antagonist to reach the market. It is orally active for the treatment of bronchospastic disorders such as asthma. TxA₂, a metabolite of the arachidonate cascade, is involved in several cardiovascular and respiratory diseases through its potent biological effects on platelet aggregation and constriction of vascular and respiratory smooth muscles. Seratrodast potently inhibits platelet aggregation and bronchoconstriction induced by a TxA₂ mimic and by a variety of spasmogenic prostanoids including PGF_2α, PGD₂ and 9α,11β-PGF₂. Seratrodast shows excellent efficacy in asthma and has been reported to be potentially useful in hyper-responsive disorder. The R-(+)- seratrodast was reported to be the active isomer.
Chemische Eigenschaften
Pale Orange Solid
Originator
Takeda (Japan)
Verwenden
Thromboxane A2-receptor antagonist. Antiasthmatic.
Verwenden
antibacterial
Definition
ChEBI: Seratrodast is an organic molecular entity.
Trademarks
Bronica
Biologische Aktivität
Thromboxane A 2 (TP) receptor antagonist. Antiasthmatic agent; inhibits platelet aggregation and bronchoconstriction induced by a TXA 2 mimetic in guinea pigs.
in vitro
seratrodast was found to inhibit the aggregation of guinea pig platelets induced by a prostaglandin endoperoxide analogue, u-44069 and the specific binding of another analogue, [3h]u-46619 to washed guinea pig platelets. seratrodast could competitively inhibit the contraction of rabbit aorta and pig coronary arteries induced by u-44069. seratrodast also inhibited the contraction of rabbit aorta induced by pgf2 alpha and the contraction of pig coronary arteries. however, seratrodast had no effect on the antiaggregatory effect of guinea pig platelets [1].
in vivo
in experiments with guinea pigs, oral seratrodast at 0.1-1 mg/kg could dose-dependently inhibit the platelet aggregation induced by u-44069; the inhibition at 1 mg/kg was 100% at 1 hr and was 89% even at 24 hr after seratrodast administration [1].
IC 50
7.4 nm for guinea pig platelets
Einzelnachweise
[1] imura, y. ,terashita, z.,shibouta, y., et al. antagonistic action of aa-2414 on thromboxane a2/prostaglandin endoperoxide receptor in platelets and blood vessels. japanese journal of pharmacology 52(1), 35-53 (1990).

Seratrodast Upstream-Materialien And Downstream Produkte

Seratrodast Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

112665-43-7, Seratrodast Verwandte Suche:

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