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Cat. No.: HY-15008

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L-368,899

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC₅₀s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.

For research use only. We do not sell to patients.

CAS No.: 148927-60-0
Formula: C₂₆H₄₂N₄O₅S₂
Molecular Weight:554.77

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

L-368,899 Chemical Structure

CAS No.: 148927-60-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (8)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 8.9 nM (rat uterus), 26 nM (human uterus)^[3].

In Vivo

L-368,899 (0.1, 0.3, 1 mg/kg; infused i.v.; single) shows a dose-related antagonism of OT-stimulated uterine contractions with an AD₅₀ value of 0.35 mg/kg in vivo^[1].
L-368,899 (3, 10, 30 mg/kg; i.d.; single) inhibits the contractile effects of OT (AD₅₀= 7 mg/kg) with a long (>4 h) duration of action in vivo (AD₅₀: the dose of L-368,899 required to reduce the response to OT by 50%)^[1].
L-368,899 (10 mg/kg, p.o.; single) shows bioavailability (AUC 0-6 h) of 35%^[1].
L-368,899 (0.54, 1.8, 5.4 mg/kg; i.v.; single) reduces both oxytocin-induced and endogenous increases in plasma PGFM concentration^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Adult female Sprague-Dawley rats (250-350 g)^[1].
Dosage:

0.1, 0.3, 1 mg/kg
Administration:

Infused intravenous injection; single.
Result:

Inhibited OT-stimulated uterine contractions with an AD₅₀ value of 0.35 mg/kg.

Animal Model:

Adult female Sprague-Dawley rats (250-350 g)^[1].
Dosage:

3, 10, 30 mg/kg
Administration:

Intraduodenal; single.
Result:

Exhibited a antagonism of OT-stimulated uterine contractions with an AD₅₀ of 7 mg/kg and duration of action more than 4 h.

Animal Model:

Adult female Sprague-Dawley rats (250-350 g)^[1].
Dosage:

10 mg/kg
Administration:

Oral administration, single.
Result:

Showed orally active with bioavailability (AUC 0-6 h) of 35%.

Animal Model:

Mature Dorset cross ewes (53-57 kg; Removal of ovaries)^[2].
Dosage:

0.54, 1.8, 5.4 mg/kg (3, 10 and 30 µg/kg/min for 3 h; dissolved in 0.9% saline).
Administration:

Intravenous infusion; single.
Result:

Led to a significant decrease in both the frequency (from 2.2 to 1.0 episodes/ewe) and amplitude (from 68.8 to 31.8 pg/mL) of episodes of increased plasma concentration of PGFM.

Chemical Information

CAS No. 148927-60-0
Molecular Weight 554.77
Formula C₂₆H₄₂N₄O₅S₂
SMILES

O=S(C[C@]12[C@H](C[C@@H](CC2)C1(C)C)NC([C@@H](N)CCS(C)(=O)=O)=O)(N3CCN(C4=C(C=CC=C4)C)CC3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (8)

All Bio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Cell

Integrating reproductive states and social cues in the control of sociosexual behaviors. [Abstract]

2025 Jun 26;188(13):3530-3549.e24. PMID: 40398420

L-368,899 purchased from MedChemExpress. Usage Cited in: Cell. 2025 Jun 26;188(13):3530-3549.e24. [Abstract]

L-368,899 hydrochloride (Oxtr antagonist) (10 mg/kg; i.p.; 20 min) treatment abolished the increased rebound activity of mPFC^Cacna1h+ neurons in estrus female mice induced by oxytocin.
Research (Wash D C)

2025 Dec 16.

L-368,899 purchased from MedChemExpress. Usage Cited in: Research (Wash D C). 2025 Dec 16.

Local application of the OXT receptor antagonist L-368,899 hydrochloride (1.25 mM; 500 nL per hemisphere) significantly reduced the peak Ca²⁺ activity of CCK neurons in CCK-Cre mice during initial interactions with a familiar mouse.
J Headache Pain

Compromised PGF2α signaling in the paraventricular hypothalamic nucleus contributes to the central sensitization of the nitroglycerin-induced chronic migraine in male mice. [Abstract]

2025 Aug 6;26(1):179. PMID: 40770605
Commun Biol

Medial prefrontal cortex neurons integrate amygdala and hypothalamic oxytocin signals to mediate stress-induced social alterations. [Abstract]

2026 Apr 23;9(1):870. PMID: 42026195
Front Pharmacol

Intradermal Injection of Oxytocin Aggravates Chloroquine-Induced Itch Responses via Activating the Vasopressin-1a Receptor/Nitric Oxide Pathway in Mice. [Abstract]

2019 Nov 15;10:1380. PMID: 31824317
Mater Technol (N Y N Y)

2025 Jun 17.
Neurosci Res

Oxytocin antagonist induced visceral pain and corticotropin-releasing hormone neuronal activation in the central nucleus of the amygdala during colorectal distention in mice. [Abstract]

2021 Jul:168:41-53. PMID: 33932549

L-368,899 purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2021 Jul:168:41-53. [Abstract]

Oxytocin antagonist L-368,899 hydrochloride (10 mg/kg; i.p.; 10 min) significantly increased the amplitudes of the VMR in C57BL/6J mice to graded CRD atall pressures compared with saline.

L-368,899 purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2021 Jul:168:41-53. [Abstract]

Oxytocin antagonist L-368,899 hydrochloride (10 mg/kg; i.p.; 10 min) significantly decreased the percentage of timespent and distance of C57BL/6J mice in open arms.

L-368,899 purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2021 Jul:168:41-53. [Abstract]

Oxytocin antagonist L-368,899 hydrochloride (10 mg/kg; i.p.; 10 min) significantly upregulated c-Fos-positive cells and c-Fos positive cells colocalized with CRH positive cells in the central amygdala (CeA) of C57BL/6J mice.
bioRxiv

2024 May 14.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pettibone D J, et al. L‐368,899, a potent orally active oxytocin antagonist for potential use in preterm labor[J]. Drug development research, 1993, 30(3): 129-142.

[2]. Mann GE, et al. Attenuation of PGF2alpha release in ewes infused with the oxytocin antagonist L-368,899. Domest Anim Endocrinol. 2003 Oct;25(3):255-62. [Content Brief]

[3]. 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 [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (8)
Purity & Documentation
References

1/16
1/16

L-368,899 purchased from MedChemExpress. Usage Cited in: Cell. 2025 Jun 26;188(13):3530-3549.e24. [Abstract]

Customer Validation
L-368,899 hydrochloride (Oxtr antagonist) (10 mg/kg; i.p.; 20 min) treatment abolished the increased rebound activity of mPFC^Cacna1h+ neurons in estrus female mice induced by oxytocin.
1/16

L-368,899 purchased from MedChemExpress. Usage Cited in: Research (Wash D C). 2025 Dec 16.

Customer Validation
Local application of the OXT receptor antagonist L-368,899 hydrochloride (1.25 mM; 500 nL per hemisphere) significantly reduced the peak Ca²⁺ activity of CCK neurons in CCK-Cre mice during initial interactions with a familiar mouse.
1/16

L-368,899 purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2021 Jul:168:41-53. [Abstract]

Customer Validation
Oxytocin antagonist L-368,899 hydrochloride (10 mg/kg; i.p.; 10 min) significantly increased the amplitudes of the VMR in C57BL/6J mice to graded CRD atall pressures compared with saline.
1/16

L-368,899 purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2021 Jul:168:41-53. [Abstract]

Customer Validation
Oxytocin antagonist L-368,899 hydrochloride (10 mg/kg; i.p.; 10 min) significantly decreased the percentage of timespent and distance of C57BL/6J mice in open arms.
1/16

L-368,899 purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2021 Jul:168:41-53. [Abstract]

Customer Validation
Oxytocin antagonist L-368,899 hydrochloride (10 mg/kg; i.p.; 10 min) significantly upregulated c-Fos-positive cells and c-Fos positive cells colocalized with CRH positive cells in the central amygdala (CeA) of C57BL/6J mice.

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L-368,899

Publications Citing Use of MedChemExpress (MCE) L-368,899