L-368,899 hydrochloride

Name: L-368,899 hydrochloride
Brand: MedChemExpress
SKU: HY-108677
Rating: 5.0 (7 reviews)

製品番号: HY-108677 純度: 99.97% ee.: 100.00%: Data Sheet SDS COA 取扱説明書
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Technical Support

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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 160312-62-9

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 254	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 254	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$110	在庫あり	Estimated Time of Arrival: December 31
5 mg	$195	在庫あり	Estimated Time of Arrival: December 31
10 mg	$310	在庫あり	Estimated Time of Arrival: December 31
25 mg	$589	在庫あり	Estimated Time of Arrival: December 31
50 mg	$940	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1500	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of L-368,899 hydrochloride:

L-368,899 お問い合わせ
L-368,899 hydrochloride (Standard) お問い合わせ

顧客検証

•bioRxiv. 2024 May 14.

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: L-368,899 hydrochloride 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.

: L-368,899 hydrochloride 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.

: L-368,899 hydrochloride 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 hydrochloride 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 hydrochloride 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.

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純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus oxytocin receptor)^[1]

体外実験

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].

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

体内実験

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].

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

分子量

591.23

分子式

C₂₆H₄₃ClN₄O₅S₂

CAS 番号

160312-62-9

Appearance

Solid

Color

White to yellow

SMILES

O=C(NC1[C@@](C2(C)C)(CS(=O)(N3CCN(C4=CC=CC=C4C)CC3)=O)CC[C@]2([H])C1)[C@H](N)CCS(=O)(C)=O.[H]Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (169.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (8.46 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6914 mL	8.4569 mL	16.9139 mL
5 mM	0.3383 mL	1.6914 mL	3.3828 mL
10 mM	0.1691 mL	0.8457 mL	1.6914 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.97% ee.: 100.00%

Select Batch:

データシート (279 KB) SDS (252 KB)

COA (256 KB) HNMR (201 KB) RP-HPLC (206 KB) NP-HPLC (144 KB) MS (229 KB)

取扱説明書 (2659 KB)

参考文献

[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 for managing preterm labor. J Med Chem. 1994 Mar 4;37(5):565-71. [Content Brief]

[2]. Kathryn L. Thompson, et al. Pharmacokinetics and Disposition of the Oxytocin Receptor Antagonist L-368,899 in Rats and Dogs

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.6914 mL	8.4569 mL	16.9139 mL	42.2847 mL
H₂O / DMSO	5 mM	0.3383 mL	1.6914 mL	3.3828 mL	8.4569 mL
DMSO	10 mM	0.1691 mL	0.8457 mL	1.6914 mL	4.2285 mL
	15 mM	0.1128 mL	0.5638 mL	1.1276 mL	2.8190 mL
	20 mM	0.0846 mL	0.4228 mL	0.8457 mL	2.1142 mL
	25 mM	0.0677 mL	0.3383 mL	0.6766 mL	1.6914 mL
	30 mM	0.0564 mL	0.2819 mL	0.5638 mL	1.4095 mL
	40 mM	0.0423 mL	0.2114 mL	0.4228 mL	1.0571 mL
	50 mM	0.0338 mL	0.1691 mL	0.3383 mL	0.8457 mL
	60 mM	0.0282 mL	0.1409 mL	0.2819 mL	0.7047 mL
	80 mM	0.0211 mL	0.1057 mL	0.2114 mL	0.5286 mL
	100 mM	0.0169 mL	0.0846 mL	0.1691 mL	0.4228 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.