| Identification | Back Directory | [Name]
(R)-2-(4'-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)aMino)-3-Methylisoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetic acid | [CAS]
1228690-19-4 | [Synonyms]
AM 966
CS-2784
AM 966; AM-966
{4'-[4-({[(1R)-1-(2-Chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]-4-biphenylyl}acetic acid
4'-[4-[[[(1R)-1-(2-Chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]-[1,1'-biphenyl]-4-acetic acid
[1,1'-BIPHENYL]-4-ACETIC ACID, 4'-[4-[[[(1R)-1-(2-CHLOROPHENYL)ETHOXY]CARBONYL]AMINO]-3-METHYL-5-ISOXAZOLYL]-
(R)-2-(4'-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)aMino)-3-Methylisoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetic acid | [Molecular Formula]
C27H23ClN2O5 | [MDL Number]
MFCD20486575 | [MOL File]
1228690-19-4.mol | [Molecular Weight]
490.93 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [Uses]
AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM). | [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. |
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BOC Sciences
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