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| 25mg |
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Purity: ≥98%
Ocaperidone (R-79598; R79598) is a potent and effective benzisoxazolyl piperidine neuroleptic and antipsychotic acting as an antagonist of 5-HT2, dopamine D2 and a 5-HT1A, with Ki values of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively.
| Targets |
5-HT2 Receptor ( Ki = 0.14 nM ); D2 Receptor ( Ki = 0.75 nM ); 5-HT1A Receptor ( pEC50 = 7.6 ); 5-HT1A Receptor ( pKi = 8.08 ); a1-adrenergic receptor ( Ki = 0.46 nM ); Histamine H1 ( Ki = 1.6 nM ); a2-adrenergic receptor ( Ki = 5.4 nM )
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| Enzyme Assay |
It uses frozen HA7 cells to prepare the membranes. Following cell harvesting, they are homogenized in ice-cold Tris-HCl pH 7.4, 4°C for 10 minutes, and then centrifuged at 40000×g. Following another centrifugation, the pellet is suspended in the same buffer. Following a second centrifugation, the pellet is suspended in an assay buffer made up of Tris-HCl (50 mM, pH 7.4), pargyline (10 μM), and CaCl2 (4 mM). The [3H] 8-OH-DPAT (1 nM final concentration) and ocaperidone at seven concentrations are incubated with membrane protein (0.031-0.084 mg/tube) for 30 minutes at room temperature. Filtration through Whatman filters stops the reaction, and liquid scintillation spectrometry measures the amount of radioactivity. Triples are used to conduct the experiments. Non-linear curve fitting software, EBDA/LIGAND, is used to analyze data. The means of three determinations are included in the results expressed as pKi values[3].
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| References |
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| Molecular Formula |
C24H25FN4O2
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| Molecular Weight |
420.49
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| Exact Mass |
420.2
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| Elemental Analysis |
C, 68.55; H, 5.99; F, 4.52; N, 13.32; O, 7.61
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| CAS # |
129029-23-8
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=CC=CN2C1=NC(=C(C2=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F)C
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| InChi Key |
ZZQNEJILGNNOEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H25FN4O2/c1-15-4-3-10-29-23(15)26-16(2)19(24(29)30)9-13-28-11-7-17(8-12-28)22-20-6-5-18(25)14-21(20)31-27-22/h3-6,10,14,17H,7-9,11-13H2,1-2H3
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| Chemical Name |
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethylpyrido[1,2-a]pyrimidin-4-one
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.97 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 16.7 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: 1.67 mg/mL (3.97 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3782 mL | 11.8909 mL | 23.7818 mL | |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7564 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 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.
Agonist activity of antipsychotics at h5-HT1Areceptors in comparison with 5-CT.Eur J Pharmacol.2001 Dec 14;433(1):55-62. |
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Correlation betweenKb/Kiratio and efficacy of antipsychotics and 5-HT1Areceptor ligands.Eur J Pharmacol.2001 Dec 14;433(1):55-62. |
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