L-365260
Based on 2 publication(s) in Google Scholar
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.85%
- CAS. Nr.: 118101-09-0
- Formel: C24H22N4O2
- Molecular Weight:398.46
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) L-365260
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Biologische Aktivität
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CCKBR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
675 nM
Compound: L-365260
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Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 3 days by MTT assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 3 days by MTT assay
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10.1039/C6MD00052E |
| MAC13 | IC50 |
>5000 nM
Compound: L-365260
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Antiproliferative activity against mouse MAC13 cells assessed as reduction in cell viability after 3 days by MTT assay
Antiproliferative activity against mouse MAC13 cells assessed as reduction in cell viability after 3 days by MTT assay
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10.1039/C6MD00052E |
| MAC16 | IC50 |
>5000 nM
Compound: L-365260
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Antiproliferative activity against mouse MAC16 cells assessed as reduction in cell viability after 3 days by MTT assay
Antiproliferative activity against mouse MAC16 cells assessed as reduction in cell viability after 3 days by MTT assay
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10.1039/C6MD00052E |
| U-373MG ATCC | IC50 |
541 nM
Compound: L-365260
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Antiproliferative activity against human U373MG cells assessed as reduction in cell viability after 3 days by MTT assay
Antiproliferative activity against human U373MG cells assessed as reduction in cell viability after 3 days by MTT assay
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10.1039/C6MD00052E |
L-365260 (1 μM) strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron[2].
L-365260 exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC50=20-40 nM) receptors in dog tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
L-365260 (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats[3].
L-365260 (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED50=0.03 mg/kg), rats (ED50=0.9 mg/kg) and guinea pigs (ED50=5.1 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (300-350 g) were injected with Morphine[3]
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Dosage:0.01, 0.05, 0.1, 0.2, 0.75, 1.0, 10.0 mg/kg
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Administration:S.c. 10 min prior to i.p. injection of 4 mg/kg Morphine
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Result:Enhanced morphine analgesia.
Chemical Information
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CAS. Nr. 118101-09-0
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Appearance Solid
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Molecular Weight 398.46
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Formel C24H22N4O2
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(C)C3=CC=CC=C3C(C4=CC=CC=C4)=N2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jan 22;189(2):640-658.e22. PMID: 41270732 -
Neuropeptides
Liangxue Tongyu prescription attenuates neuroinflammation by increasing cholecystokinin octapeptide in acute intracerebral hemorrhage rats. [Abstract]2024 Jun 24:107:102452. PMID: 38941823
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (250.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.27 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lotti VJ, et, al. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. [Content Brief]
[2]. Chung L, et, al. Cholecystokinin action on layer 6b neurons in somatosensory cortex. Brain Res. 2009 Jul 28;1282:10-9. [Content Brief]
[3]. Dourish CT, et, al. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Eur J Pharmacol. 1990 Jan 25;176(1):35-44. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5097 mL | 12.5483 mL | 25.0966 mL | 62.7416 mL |
| 5 mM | 0.5019 mL | 2.5097 mL | 5.0193 mL | 12.5483 mL | |
| 10 mM | 0.2510 mL | 1.2548 mL | 2.5097 mL | 6.2742 mL | |
| 15 mM | 0.1673 mL | 0.8366 mL | 1.6731 mL | 4.1828 mL | |
| 20 mM | 0.1255 mL | 0.6274 mL | 1.2548 mL | 3.1371 mL | |
| 25 mM | 0.1004 mL | 0.5019 mL | 1.0039 mL | 2.5097 mL | |
| 30 mM | 0.0837 mL | 0.4183 mL | 0.8366 mL | 2.0914 mL | |
| 40 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5685 mL | |
| 50 mM | 0.0502 mL | 0.2510 mL | 0.5019 mL | 1.2548 mL | |
| 60 mM | 0.0418 mL | 0.2091 mL | 0.4183 mL | 1.0457 mL | |
| 80 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7843 mL | |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6274 mL |
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