| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In many neurons, CCK8S- and CCK4-mediated depolarization is significantly attenuated by L-365260 (1 μM) [2]. For CCK-B receptors in the brains of rats, mice, and humans, L-365260 demonstrates a comparable high affinity, whereas its affinity for gastrin and brain CCK-B (IC50=20–40 nM) receptors in dog tissue is lower[1].
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|---|---|
| ln Vivo |
Rats given submaximal doses of morphine (4 mg/kg) experience analgesia that is potentiated by L-365260 (0.01-10 mg/kg; subcutaneous injection) [3]. In rats, the duration of morphine analgesia was greatly extended by L-365260 (0.2 mg/kg; subcutaneous injection twice daily for 5 days) [3]. Gastrin enhancement of acid secretion in mice (ED50=0.03 mg/kg), rats (ED50=0.9 mg/kg), and guinea pigs (ED50=5.1 mg/kg) is antagonized by L-365260 (0.1-30 mg/kg; po)[1].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (300-350 g) injected with morphine [3]
Doses: 0.01, 0.05, 0.1, 0.2, 0.75, 1.0, 10.0 mg/kg Route of Administration: 10 minutes before subcutaneous injection 4 mg/kg Morphine Experimental Results: The analgesic effect of morphine is enhanced. |
| References |
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| Additional Infomation |
L-365260 is a benzodiazepine.
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| Molecular Formula |
C24H22N4O2
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|---|---|
| Molecular Weight |
398.47
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| Exact Mass |
398.174
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| CAS # |
118101-09-0
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| Related CAS # |
L-365260 hemihydrate
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| PubChem CID |
5311201
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| Appearance |
White to off-white solid powder
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| Density |
1.23g/cm3
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| Boiling Point |
611.5ºC at 760 mmHg
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| Flash Point |
323.6ºC
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| Vapour Pressure |
6.85E-15mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
3.921
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
658
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CC(=CC=C1)NC(=O)N[C@H]2C(=O)N(C3=CC=CC=C3C(=N2)C4=CC=CC=C4)C
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| InChi Key |
KDFQABSFVYLGPM-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C24H22N4O2/c1-16-9-8-12-18(15-16)25-24(30)27-22-23(29)28(2)20-14-7-6-13-19(20)21(26-22)17-10-4-3-5-11-17/h3-15,22H,1-2H3,(H2,25,27,30)/t22-/m0/s1
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| Chemical Name |
1-[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea
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| Synonyms |
L365260; L 365260; L-365260
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~250.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5096 mL | 12.5480 mL | 25.0960 mL | |
| 5 mM | 0.5019 mL | 2.5096 mL | 5.0192 mL | |
| 10 mM | 0.2510 mL | 1.2548 mL | 2.5096 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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