| Bioactivity | L-368,899 hydrochloride is a potent, selective, 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 hydrochloride used as a tocolytic agent[1]. |
| Target | IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus oxytocin receptor) |
| Invitro | 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)[1]. |
| In Vivo | 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[2].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[2]. |
| Name | L-368,899 hydrochloride |
| CAS | 160312-62-9 |
| Formula | C26H43ClN4O5S2 |
| Molar Mass | 591.23 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Williams PD, 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 fo [2]. Kathryn L. Thompson, et al. Pharmacokinetics and Disposition of the Oxytocin Receptor Antagonist L-368,899 in Rats and Dogs |
L-368,899 hydrochloride
CAS: 160312-62-9 F: C26H43ClN4O5S2 W: 591.23
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50
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