Bioactivity | 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.) 可以延缓 RU486 引起的早产。也可以剂量依赖性抑制 GD14 触发的分娩,在 30 mg/kg 和 100 mg/kg 的剂量下,平均分娩时间分别显着增加 16.5 和 33.5 小时。而对 GD17 引产的分娩延迟作用不太显着[1]。AS604872 (3-120 mg/kg, i.v.) 可以以剂量依赖性方式抑制 PGF 2α 引发的磷酸肌醇的总合成,并显着降低 PGF 2α在 SD BR 非妊娠雌性大鼠中引起的子宫收缩,在 60 mg/kg 时的最大作用为 27%。同时也能够抑制孕鼠的自发性子宫收缩[1]。 |
Name | AS604872 |
CAS | 612532-48-6 |
Formula | C28H25N3O3S2 |
Molar Mass | 515.65 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |