L-365260 hemihydrate
Based on 2 publication(s) in Google Scholar
L-365260 hemihydrate 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 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.
For research use only. We do not sell to patients.
- Purity: 99.75%
- Formula: C24H24N4O3
- Molecular Weight:407.47
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) L-365260 hemihydrate
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Biological Activity
Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B)[1].
L-365260 hemihydrate 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].
L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats[3].
L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats[3].
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; Morphine- injected)[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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Appearance Solid
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Molecular Weight 407.47
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Formula C24H24N4O3
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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.[1/2].O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 Oct:107:102452. PMID: 38941823
Solvent & Solubility
DMSO : 50 mg/mL (122.71 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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]. 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]
[3]. 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]
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 (sealed storage, away from moisture). 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 | 2.4542 mL | 12.2708 mL | 24.5417 mL | 61.3542 mL |
| 5 mM | 0.4908 mL | 2.4542 mL | 4.9083 mL | 12.2708 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4542 mL | 6.1354 mL | |
| 15 mM | 0.1636 mL | 0.8181 mL | 1.6361 mL | 4.0903 mL | |
| 20 mM | 0.1227 mL | 0.6135 mL | 1.2271 mL | 3.0677 mL | |
| 25 mM | 0.0982 mL | 0.4908 mL | 0.9817 mL | 2.4542 mL | |
| 30 mM | 0.0818 mL | 0.4090 mL | 0.8181 mL | 2.0451 mL | |
| 40 mM | 0.0614 mL | 0.3068 mL | 0.6135 mL | 1.5339 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.2271 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0226 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3068 mL | 0.7669 mL | |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 mL |
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