ONO-7300243 Property

Boiling point:

688.1±55.0 °C(Predicted)

Density 

1.180±0.06 g/cm3(Predicted)

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

≥46.1 mg/mL in DMSO; insoluble in H2O; ≥11.55 mg/mL in EtOH with ultrasonic

form 

solid

pka

4.30±0.10(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

ONO-7300243 Chemical Properties,Usage,Production

Biological Activity

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

IC 50

160 nm

References

[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.