L-368,899 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

L-368,899 盐酸盐是一种有效的、选择性的、口服生物可利用的、非肽催产素受体拮抗剂，用作宫缩剂时，对大鼠子宫和人子宫催产素受体的 IC50 值分别为 8.9 nM 和 26 nM。

L-368,899 hydrochloride is a potent, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s 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 (IC50, 510 nM, 960 nM, 890 nM, 2400 nM, respectively).

L-368,899 hydrochloride is a potent, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s 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 (IC50, 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 t1/2 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 Vdss 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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GPCR/G Protein

Orexin Receptor

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160312-62-9

591.23

C??H??ClN?O?S?

>98% (HPLC)

DMSO : 130 mg/mL (219.88 mM; Need ultrasonic)

O=C(NC1[C@@](C2(C)C)(CS(=O)(N3CCN(C4=CC=CC=C4C)CC3)=O)CC[C@]2([H])C1)[C@H](N)CCS(=O)(C)=O.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years