L-368,899 HYDROCHLORIDE
中文名称 | L-368,899 HYDROCHLORIDE |
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中文同义词 | 化合物 T11794;L-368,899盐酸盐 |
英文名称 | 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 |
英文同义词 | 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;L-368,899 HYDROCHLORIDE;(S)-2-amino-N-((1S,2S,4R)-7,7-dimethyl-1-(((4-(o-tolyl)piperazin-1-yl)sulfonyl)methyl)bicyclo[2.2.1]heptan-2-yl)-4-(methylsulfonyl)butanamide hydrochloride;899 hydrochloride;L-368 |
CAS号 | 160312-62-9 |
分子式 | C26H42N4O5S2 |
分子量 | 554.77 |
EINECS号 | |
相关类别 | |
Mol文件 | Mol File |
结构式 |
L-368,899 HYDROCHLORIDE 性质
储存条件 | −20°C |
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溶解度 | H2O:20 mg/mL,可溶 |
形态 | 粉末 |
颜色 | 白色 |
IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus oxytocin receptor)
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).
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.
安全信息
安全说明 | 22-24/25 |
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WGK Germany | 3 |
提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-108677 | L-368,899 HYDROCHLORIDE L-368,899 hydrochloride | 160312-62-9 | 1mg | 1000元 |
2024/01/25 | HY-108677 | L-368,899 HYDROCHLORIDE L-368,899 hydrochloride | 160312-62-9 | 5mg | 1900元 |