ChemicalBook > CAS DataBase List > 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

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
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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
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Safety

Safety Statements 
22-24/25
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
L2540
Product name
L-<SC>368,899</SC>
Purity
&#8805;98% (HPLC), powder
Packaging
5 mg
Price
$694
Updated
2025/07/31
Cayman Chemical
Product number
29868
Product name
L-368,899 (hydrochloride)
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
29868
Product name
L-368,899 (hydrochloride)
Packaging
10mg
Price
$356
Updated
2024/03/01
Cayman Chemical
Product number
29868
Product name
L-368,899 (hydrochloride)
Packaging
5mg
Price
$227
Updated
2024/03/01
Tocris
Product number
2641
Product name
L-368,899hydrochloride
Purity
≥97%(HPLC)
Packaging
10
Price
$330
Updated
2021/12/16
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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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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 Suppliers

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160312-62-9, 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 HYDROCHLORIDERelated Search:


  • 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
  • 899 hydrochloride
  • L-368
  • L-<sc>368,899</sc>
  • 160312-62-9