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50mg |
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100mg |
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Other Sizes |
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Olanzapine/Samidorphan is a combination therapy composed of olanzapine and the opioid receptor antagonist samidorphan. The combination therapy is under development for the treatment of schizophrenia and bipolar I disorder. The single-tablet combination treatment is intended to provide the efficacy of olanzapine while mitigating olanzapine-associated weight gain.
ln Vitro |
Olanzapine can be absorbed (Ki>10 μM) and binds weakly to GABAA, azepine (BZD), and β-prosin[1][2]. The human SH-SY5Y neural cell line exhibits autophagy in response to olanzapine [3]. Astrocytoblastoma cells and astrocytoma stem-like cells are significantly inhibited from proliferating when exposed to 1-100 μM and serum-starved for 144 hours [4]. Olanzapine improved the antitumor effects on cell lines that mimic astrocytes.
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ln Vivo |
Mice's body weight, periuterine fat mass, insulin, non-esterified medium, triglyceride, and blood glucose levels were assessed using olanzapine (0.75, 1.5, and 3 mg/kg) [5].
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Cell Assay |
Cell Proliferation Assay[4]
Cell Types: U87MG and A172 glioblastoma cell lines and SC38 and SC40 glioma stem cell-like cell activity[4]. Tested Concentrations: 1, 10, 100 μM Incubation Duration: 144 hrs (hours); performed under serum starvation (1.5% FBS) before MTT assay Experimental Results: Produced significant antiproliferative effect with IC50 values ranging from 25 to 79.9 µM. In U87MG cells, anchorage-independent growth was dose-dependently inhibited. In A172 cells, migration was also shown to be inhibited in a dose-dependent manner. Western Blot Analysis [4] Cell Types: U87MG and A172 Cell Tested Concentrations: 10, 25, 50 and 100 μM Incubation Duration: 7 hrs (hours), 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Result in a dose-responsive decrease in pAMPK expression after treatment for 72 hrs (hours). |
Animal Protocol |
Animal/Disease Models: 42, 14, and 28 female CD-1 mice [5]
Doses: 0.75, 1.5, and 3 mg/kg Route of Administration: oral and chronic administration; 35-day Experimental Results: Day 20-22, relative Compared to vehicle, body weight increased, starting on day 32, directly at 3 mg/kg. No differences were found between the control group and mice administered 1.5 and 0.75 mg/kg olanzapine. |
References |
[1]. APPROVED AGREED-UPON LABELING.
[2]. Olanzapine for Injection, powder, for solution for intramuscular use. [3]. Vucicevic L, et al. Autophagy inhibition uncovers the neurotoxic action of the antipsychotic drug olanzapine. Autophagy. 2014;10(12):2362-78. [4]. Karpel-Massler G, et al. Olanzapine inhibits proliferation, migration and anchorage-independent growth in human glioblastoma cell lines and enhances temozolomide's antiproliferative effect. J Neurooncol. 2015 Mar;122(1):21-33. [5]. Coccurello R, et al. Chronic administration of olanzapine induces metabolic and food intake alterations: a mousemodel of the atypical antipsychotic-associated adverse effects. Psychopharmacology (Berl). 2006 Jul;186(4):561-71. |
Molecular Formula |
C17H20N4S
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Molecular Weight |
312.43
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CAS # |
132539-06-1
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Related CAS # |
Olanzapine-d3;786686-79-1
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SMILES |
S1C(C([H])([H])[H])=C([H])C2=C1N([H])C1=C([H])C([H])=C([H])C([H])=C1N=C2N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H]
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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 : ~20 mg/mL (~64.01 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (6.40 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 20.0 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 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.0 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. View More
Solubility in Formulation 3: ≥ 2 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2007 mL | 16.0036 mL | 32.0072 mL | |
5 mM | 0.6401 mL | 3.2007 mL | 6.4014 mL | |
10 mM | 0.3201 mL | 1.6004 mL | 3.2007 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.