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160312-62-9

中文名称 L-368,899 HYDROCHLORIDE
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
CAS 160312-62-9
分子式 C26H42N4O5S2
分子量 554.77
MOL 文件 160312-62-9.mol
更新日期 2024/09/02 21:45:13
160312-62-9 结构式 160312-62-9 结构式

基本信息

中文别名
化合物 T11794
L-368,899盐酸盐
英文别名
L-368,899 HYDROCHLORIDE
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

物理化学性质

储存条件−20°C
储存条件−20°C
溶解度H2O: 20 mg/mL, soluble
溶解度H2O:20 mg/mL,可溶
形态powder
颜色white

安全数据

安全说明22-24/25
WGK Germany3
WGK Germany3
L-368,899 HYDROCHLORIDE价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-108677L-368,899 HYDROCHLORIDE
L-368,899 hydrochloride
160312-62-91mg1000元
2024/08/19HY-108677L-368,899 HYDROCHLORIDE
L-368,899 hydrochloride
160312-62-95mg1900元
2024/08/19HY-108677L-368,899 HYDROCHLORIDE
L-368,899 hydrochloride
160312-62-910mM * 1mLin DMSO2471元

常见问题列表

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).

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.

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