| Description | L-368,899 hydrochloride is an orally available and selective nonpeptide oxytocin receptor (OXTR) antagonist for the prevention of preterm labor.L-368,899 hydrochloride prevents oxytocin-induced anti-anomalous pain and anti-nausea, and may be useful for the study of depression. |
| In vitro | L-368,899 hydrochloride 是有效的非肽类催产素受体拮抗剂，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[1]。 |
| In vivo | L-368,899 （5 mg/kg；口服）在雌性和雄性大鼠的口服生物利用度分别为 14% 和 18%[2]。 |
| Target activity | OTR (human uterus):26 nM, OTR (rat uterus):8.9 nM |
| Synonyms | L-368899 hydrochloride, L-368,899 HCl |
| molecular weight | 591.23 |
| Molecular formula | C26H43ClN4O5S2 |
| CAS | 160312-62-9 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 2 mg/mL (3.38 mM), Sonication is recommended. DMSO: 100 mg/mL (169.14 mM), Sonication is recommended. |
| References | 1. Williams PD, Anderson PS, Ball RG, Bock MG, Carroll L, Chiu SH, Clineschmidt BV, Culberson JC, Erb JM, Evans BE, et al. 1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor. J Med Chem. 1994 Mar 4;37(5):565-71. 2. Thompson KL, et al. Pharmacokinetics and disposition of the oxytocin receptor antagonist L-368,899 in rats and dogs. Drug Metab Dispos. 1997 Oct;25(10):1113-8. |