L-368,899 HYDROCHLORIDE
- CAS号:160312-62-9
- 英文名:1-((7,7-DIMETHYL-2(S)-(2(S)-AMINO-4-(METHYLSULFONYL)BUTYRAMIDO)BICYCLO[2,2,1]HEPTAN-1(S)-YL)METHYLSULFONYL)-4-(2-METHYLPHENYL)PIPERAZINE HYDROCHLORIDE
- 中文名:L-368,899 HYDROCHLORIDE
- CBNumber:CB6302164
- 分子式:C26H42N4O5S2
- 分子量:554.77
- MOL File:Mol file
- 储存条件 :−20°C
- 溶解度 :H2O: 20 mg/mL, soluble
- 形态 :powder
- 颜色 :white
- 安全说明 :22-24/25
- WGK Germany :3
L-368,899 HYDROCHLORIDE性质、用途与生产工艺
- 生物活性 L-368,899 hydrochloride 是一种有效的,选择性的,可口服的,非肽类催产素受体 oxytocin receptor 拮抗剂,对大鼠和人子宫 oxytocin receptor 的 IC50 值分别为 8.9 nM 和 26 nM,为抗早产剂。
-
靶点
IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus oxytocin receptor)
-
体外研究
L-368,899 hydrochloride is a potent, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC 50 s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 is less active on VP receptor in human liver and kidney, rat liver and kidney (IC 50 , 510 nM, 960 nM, 890 nM, 2400 nM, respectively).
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体内研究
L-368,899 exhibits similar pharmacokinetics in rats and dogs. After a single iv. injection, L-368,899 had a t 1/2 of 2 hr in both species. Additionally, L-368,899 has a plasma clearance between 23 and 36 ml/min/kg in rats or dogs. L-368,899 exhibits V dss values of 2.0 and 2.6 liters/kg and 3.4 to 4.9 liters/kg for dogs, respectively. L-368,899 is orally available. In the rat, at the 5 mg/kg dose, the oral bioavailabilities are 14% and 18% for female and male rats, respectively. Additionally, the oral bioavailabilities are 17% and 41% for female and male rats, respectively at the dosage of 25 mg/kg.
- 更新日期:2024/01/25
- 产品编号:HY-108677
- 产品名称:L-368,899 HYDROCHLORIDE L-368,899 hydrochloride
- CAS编号:160312-62-9
- 包装:1mg
- 价格:1000元
- 更新日期:2024/01/25
- 产品编号:HY-108677
- 产品名称:L-368,899 HYDROCHLORIDE L-368,899 hydrochloride
- CAS编号:160312-62-9
- 包装:5mg
- 价格:1900元
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