2. GPCR/G Protein
  3. Oxytocin Receptor
  4. L-368,899

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。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 L-368,899 hydrochloride 通常具有更好的水溶性和稳定性。

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L-368,899 Chemical Structure

L-368,899 Chemical Structure

CAS No. : 148927-60-0

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L-368,899 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s 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 AD50 value 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 AD50 value 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 AD50 of 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
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.
纯度 & 产品资料
参考文献

L-368,899 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-368,899148927-60-0Oxytocin ReceptorOXTROTPGF2αPGFMpreterm laboruterine contractionsInhibitorinhibitorinhibit

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