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: ≥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: 1
Price: $154
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 V_1a 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 t_1/2 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 V_dss 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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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