ONO-7300243 Struktur

ONO-7300243

Bezeichnung:ONO-7300243

CAS-Nr638132-34-0

Englisch Name:ONO-7300243

CBNumberCB53155069

SummenformelC28H31NO5

Molgewicht461.55

MOL-Datei638132-34-0.mol

ONO-7300243 physikalisch-chemischer Eigenschaften

Siedepunkt	688.1±55.0 °C(Predicted)
Dichte	1.180±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	≥46.1 mg/mL in DMSO; insoluble in H2O; ≥11.55 mg/mL in EtOH with ultrasonic
Aggregatzustand	solid
pka	4.30±0.10(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

ONO-7300243 Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
ono-7300243 is a lpa1 antagonist.lysophosphatidic acids (lpas), a bioactive class of phospholipids, are produced by autotaxin from lysophosphatidylcholine in blood. lpas have a wide range of cellular responses, such as cell proliferation, intracellular ca2+ mobilization, cell survival, and cell motility. based on their specific properties, lpas have been involved in various complex physiological responses, such as the contraction of smooth muscle, wound healing, coagulation, demyelization, as well as immunological competence.
in vitro
ono-7300243 was identified as a novel and potent lpa1 antagonist. importantly, it was found that ono-7300243 showed equal potency to the α1 adrenoceptor antagonist tamsulosin that is clinically used for the treatment of dysuria with benign prostatic hyperplasia (bph) [1].
in vivo
animal study reported that although ono-7300243 showed only modest in vitro activity (ic50 = 0.16 μm), the oral dosing of ono-7300243 to rats resulted in much stronger effects on reducing intraurethral pressure (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.). when compared with tamsulosin, ono-7300243 had no effect on the mean blood pressure at this dose, which suggested that lpa1 antagonists could be used to treat bph without affecting the blood pressure [1].
target

IC50: 0.19-0.13 μM (LPA1)
IC 50
160 nm
Einzelnachweise
[1] terakado m et al. discovery of ono-7300243 from a novel class of lysophosphatidic acid receptor 1 antagonists: from hit to lead. acs med chem lett. 2016 aug 19;7(10):913-918. ecollection 2016.

ONO-7300243 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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