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L-368,899
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-368,899图片
CAS NO:148927-60-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
L-368,899 是一种口服有效的选择性催产素受体 oxytocin receptor 拮抗剂,对大鼠和人子宫 oxytocin receptor 的IC50值分别为 8.9 和 26 nM。L-368,899 可穿过血脑屏障。L-368,899 能抑制大鼠和恒河猴中催产素刺激的子宫收缩,可用于早产的研究。
生物活性

L-368,899 is an orally active and selectiveOT (oxytocin ) receptorantagonist, withIC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor[1][2][3].

IC50& Target

IC50: 8.9 nM (rat uterus), 26 nM (human uterus)[3].

体内研究
(In Vivo)

L-368,899 (0.1, 0.3, 1 mg/kg; infused i.v.; single) shows a dose-related antagonism of OT-stimulated uterine contractions with an AD50value of 0.35 mg/kg in vivo[1].
L-368,899 (3, 10, 30 mg/kg; i.d.; single) inhibits the contractile effects of OT (AD50= 7 mg/kg) with a long (>4 h) duration of action in vivo (AD50: the dose of L-368,899 required to reduce the response to OT by 50%)[1].
L-368,899 (10 mg/kg, p.o.; single) shows bioavailability (AUC 0-6 h) of 35%[1].
L-368,899 (0.54, 1.8, 5.4 mg/kg; i.v.; single) reduces both oxytocin-induced and endogenous increases in plasma PGFM concentration[2].

Animal Model:Adult female Sprague-Dawley rats (250-350 g)[1].
Dosage:0.1, 0.3, 1 mg/kg
Administration:Infused intravenous injection; single.
Result:Inhibited OT-stimulated uterine contractions with an AD50value of 0.35 mg/kg.
Animal Model:Adult female Sprague-Dawley rats (250-350 g)[1].
Dosage:3, 10, 30 mg/kg
Administration:Intraduodenal; single.
Result:Exhibited a antagonism of OT-stimulated uterine contractions with an AD50of 7 mg/kg and duration of action more than 4 h.
Animal Model:Adult female Sprague-Dawley rats (250-350 g)[1].
Dosage:10 mg/kg
Administration:Oral administration, single.
Result:Showed orally active with bioavailability (AUC 0-6 h) of 35%.
Animal Model:Mature Dorset cross ewes (53-57 kg; Removal of ovaries)[2].
Dosage:0.54, 1.8, 5.4 mg/kg (3, 10 and 30 μg/kg/min for 3 h; dissolved in 0.9% saline).
Administration:Intravenous infusion; single.
Result:Led to a significant decrease in both the frequency (from 2.2 to 1.0 episodes/ewe) and amplitude (from 68.8 to 31.8 pg/mL) of episodes of increased plasma concentration of PGFM.
分子量

554.77

Formula

C26H42N4O5S2

CAS 号

148927-60-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.