| Identification | Back Directory | [Name]
2-Thiazolidinecarboxamide, 3-([1,1'-biphenyl]-4-ylsulfonyl)-N-[(R)-phenyl-2-pyridinylmethyl]-, (2S)- | [CAS]
612532-48-6 | [Synonyms]
AS604872
AS-604872
AS 604872
2-Thiazolidinecarboxamide, 3-([1,1'-biphenyl]-4-ylsulfonyl)-N-[(R)-phenyl-2-pyridinylmethyl]-, (2S)- | [Molecular Formula]
C28H25N3O3S2 | [MOL File]
612532-48-6.mol | [Molecular Weight]
515.65 |
| Hazard Information | Back Directory | [Description]
AS604872 is a small molecule selective antagonist of the FP receptor in inhibition of spontaneous uterine contraction. AS604872 significantly accelerated degeneration of the media in both cerebral artery and aorta as evidenced by thinning of the media and disruption of the elastic lamina and promoted IA and aortic dissection. AS604872 can be used to make models of these vascular diseases with extensive degeneration. | [Uses]
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour[1]. | [in vivo]
AS604872 (10-100 mg/kg, p.o.)?delays RU486-induced preterm labour. It also dose-dependently inhibits GD14-triggered labour, with a significant increase in mean time to delivery of 16.5 and 33.5 hours at 30 mg/kg and 100 mg/kg, respectively. However, the delayed effect on GD17-induced labour is less pronounced in mice[1].
AS604872 (3-120 mg/kg, i.v.)?inhibits PGF 2α-triggered total synthesis of phosphatidylinositol in a dose-dependent manner and significantly reduces PGF 2α-induced uterine contractions in SD BR non-pregnant female rats, with a maximum effect of 27% at 60 mg/kg. It also inhibited spontaneous uterine contractions in pregnant rats[1].
| [References]
[1] Rocco Cirillo, et al. Arrest of preterm labor in rat and mouse by an oral and selective nonprostanoid antagonist of the prostaglandin F2alpha receptor (FP). Am J Obstet Gynecol. 2007 Jul;197(1):54.e1-9. DOI:10.1016/j.ajog.2007.02.010 |
|
|