(R)-2-(4'-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)aMino)-3-Methylisoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetic acid Property

Boiling point:

659.4±55.0 °C(Predicted)

Density 

1.330±0.06 g/cm3 (20 ºC 760 Torr)

storage temp. 

Store at -20°C

solubility 

≥24.55 mg/mL in DMSO; insoluble in H2O; ≥2.24 mg/mL in EtOH with gentle warming and ultrasonic

form 

solid

pka

4.21±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.

(R)-2-(4'-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)aMino)-3-Methylisoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetic acid Chemical Properties,Usage,Production

Biological Activity

am966 is a selective, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (lpa1) with ic50 values of 17 and 19 nm for human or mouse lpa1, respectively [1]. relative to lpa2, 3, 4, 5 receptors, am966 shows 10-fold and 100-fold more selective in mouse and human cell lines for lpa1, respectively [1].

in vitro

am966 shows to inhibit lpa-induced chemotaxis in imr-90 human lung fibroblasts, a2058 human melanoma cells and cho cells expressing lpa1 receptors [1].

in vivo

am966 has been demonstrated to reduce total balf cells, ldh activity, balf collagen and total tgfβ concentrations in bleomycin-induced mice. moreover, am966 has been reported to block lung fibrosis, reduce lung inflammation and maintain body weight in mice induced by bleomycin [1].

target

LPA1 receptor

References

[1] swaney js1, chapman c, correa ld, stebbins kj, bundey ra, prodanovich pc, fagan p, baccei cs, santini am, hutchinson jh, seiders tj,parr ta, prasit p, evans jf, lorrain ds. a novel, orally active lpa(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. br j pharmacol. 2010 aug;160(7):1699-713.