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
- Product Name
- 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 No.
- 160312-62-9
- Chemical Name
- 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
- Synonyms
- L-368;899 hydrochloride;L-
368,899 ;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;(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 - CBNumber
- CB6302164
- Molecular Formula
- C26H42N4O5S2
- Formula Weight
- 554.77
- MOL File
- Mol file
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 Property
- storage temp.
- −20°C
- solubility
- H2O: 20 mg/mL, soluble
- form
- powder
- color
- white
- Water Solubility
- H2O: soluble 20mg/mL
Safety
- Safety Statements
- 22-24/25
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- L2540
- Product name
- L-<SC>368,899</SC>
- Purity
- ≥98% (HPLC), powder
- Packaging
- 5 mg
- Price
- $694
- Updated
- 2025/07/31
- Product number
- 29868
- Product name
- L-368,899 (hydrochloride)
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 29868
- Product name
- L-368,899 (hydrochloride)
- Packaging
- 10mg
- Price
- $356
- Updated
- 2024/03/01
- Product number
- 29868
- Product name
- L-368,899 (hydrochloride)
- Packaging
- 5mg
- Price
- $227
- Updated
- 2024/03/01
- Product number
- 2641
- Product name
- L-368,899hydrochloride
- Purity
- ≥97%(HPLC)
- Packaging
- 10
- Price
- $330
- Updated
- 2021/12/16
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 Chemical Properties,Usage,Production
Description
L-368,899 is a non-peptide oxytocin receptor antagonist (IC50s = 8.9 and 26 nM in radioligand binding assays using isolated human and rat uterus, respectively). It is selective for oxytocin receptors over vasopressin V1a and V2 receptors (IC50s = 370 and 570 nM, respectively). L-368,899 reduces oxytocin-induced contraction of isolated rat uterus (pA2 = 8.9) and in situ rat uterus (ED50 = 0.35 mg/kg, i.v.).
Uses
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].
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].
storage
Store at -20°C
References
[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 DOI:10.1021/jm00031a004
[2] Kathryn L. Thompson, et al. Pharmacokinetics and Disposition of the Oxytocin Receptor Antagonist L-368,899 in Rats and Dogs
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 Preparation Products And Raw materials
Raw materials
Preparation Products
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