Olanzapine
Based on 14 publication(s) in Google Scholar
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 132539-06-1
- Formula: C17H20N4S
- Molecular Weight:312.44
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Olanzapine
More- Nat Commun. 2022 Nov 10;13(1):6796. [Abstract]
- Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Brain Pathol. 2024 Sep 18:e13306. [Abstract]
- Front Pharmacol. 2022 Aug 12:13:935362. [Abstract]
- ACS Omega. 2025 Oct 17;10(42):50208-50217. [Abstract]
- Drug Dev Res. 2024 Jun;85(4):e22225. [Abstract]
- Toxicol Appl Pharmacol. 2025 Sep 10:505:117551. [Abstract]
- Patent. US20250295610A1.
- University of South Carolina. 2025.
- Research Square Print. 2022 Aug.
- medRxiv. 2021 Mar 1.
- bioRxiv. 2021 Mar 02.
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Cell Proliferation/Viability Assay
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ELISA
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WB
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Histological Imaging/Staining
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RT-PCR
All 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
MoreAll Adrenergic Receptor Isoforms
More
Biological Activity
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5-HT2A Receptor 4 nM (Ki) |
5-HT2A Receptor |
5-HT6 Receptor |
5-HT1 Receptor 7 nM (Ki) |
5-HT6 Receptor 5 nM (Ki) |
5-HT2C Receptor 11 nM (Ki) |
5-HT3 Receptor 57 nM (Ki) |
Adrenergic α1 Receptor 19 nM (Ki) |
Muscarinic M1-5 Receptor 1.9-25 nM (Ki) |
Dopamine Receptor |
Mitophagy |
Apoptosis |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.173 μM
Compound: olanzapine
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Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells
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[PMID: 8831770] |
| HEK293 | IC50 |
0.1 μM
Compound: Olanzapine
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Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
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[PMID: 26227779] |
| RAW264.7 | CC50 |
198.3 μM
Compound: Olanzapine
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Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 38283231] |
| WI-38 | CC50 |
>100 μM
Compound: Olanzapine
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Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
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[PMID: 17893158] |
| WI-38 | EC50 |
>100 μM
Compound: Olanzapine
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Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
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[PMID: 17893158] |
Olanzapine binds weakly to GABAA, Benzodiazepine (BZD), and β-adrenergic receptors (Ki>10 μM) [1][2].
Olanzapine induces autophagy in human SH-SY5Y neuronal cell line[3].
Olanzapine (1-100 μM for 144 h under serum starvation) results in a marked anti-proliferative effect in glioblastoma cell lines as well as glioma stem-like cells[4].
Olanzapine also enhances Temozolomide (HY-17364)’s anti-tumor activity in glioblastoma cell lines[4].
Olanzapine induces apoptosis and necrosis in glioblastoma cell lines[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87MG and A172 glioblastoma cell lines as well as SC38 and SC40 glioma stem-like cells
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Concentration:1, 10, 100 μM
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Incubation Time:144 h; under serum starvation (1.5 % FBS) prior to performing MTT-assays
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Result:Resulted in a marked 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.
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Cell Line:U87MG and A172 cells
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Concentration:10, 25, 50, and 100 μM
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Incubation Time:7 h, 24 h, 48 h, 72 h
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Result:Led to a dose responsive decrease of pAMPK expression after 72 h of treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Forty-two, 14, and 28 female CD-1 mice [5]
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Dosage:0.75, 1.5 and 3 mg/kg
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Administration:Orally and chronically administered; 35 days
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Result:Increased body weight relative to vehicle on days 20-22, and from day 32 onwards there was a straightforward increase in body weight at 3 mg/kg. No differences were found between control and mice administered olanzapine at both 1.5 and 0.75 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 132539-06-1
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Appearance Solid
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Molecular Weight 312.44
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Formula C17H20N4S
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Color Light yellow to yellow
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SMILES
CC1=CC(C(N2CCN(C)CC2)=N3)=C(S1)NC4=C3C=CC=C4
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Synonyms
LY170053
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
Maprotiline restores ER homeostasis and rescues neurodegeneration via Histamine Receptor H1 inhibition in retinal ganglion cells. [Abstract]2022 Nov 10;13(1):6796. PMID: 36357388
Olanzapine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 10;13(1):6796. [Abstract]
Relative CHOP-Luc activities of individual tested compounds (Olanzapine) at 20 µM in the presence of Tm/Tg (1 µM) relative to DMSO, 24 hours after exposure.
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Acta Pharmacol Sin
Brexpiprazole caused glycolipid metabolic disorder by inhibiting GLP1/GLP1R signaling in rats. [Abstract]2021 Aug;42(8):1267-1279. PMID: 33976388
Olanzapine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
Olanzapine (Ola: 1.0 mg/kg). Serum insulin-metabolizing hormone levels were measured using a commercially available enzyme-linked immunosorbent assay (ELISA) kit.
Olanzapine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
Olanzapine (Ola: 1.0 mg/kg). The expression level of GLP-1 protein in small intestinal tissue was detected by Western blot analysis.
Olanzapine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
Olanzapine (Ola: 1.0 mg/kg). GLP-1 immunohistochemical staining was performed on paraffin sections of the small intestine.
Olanzapine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
Olanzapine (Ola: 1.0 mg/kg). The mRNA expression level in liver tissue was detected using real-time quantitative PCR.
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Brain Pathol
2024 Sep 18:e13306. PMID: 39293934 -
Front Pharmacol
Alterations in sorting and secretion of hepatic apoA5 induce hypertriglyceridemia due to short-term use of olanzapine. [Abstract]2022 Aug 12:13:935362. PMID: 36034782 -
ACS Omega
2025 Oct 17;10(42):50208-50217. PMID: 41179162 -
Drug Dev Res
SEP-363856 exerts neuroprotection through the PI3K/AKT/GSK-3β signaling pathway in a dual-hit neurodevelopmental model of schizophrenia-like mice. [Abstract]2024 Jun;85(4):e22225. PMID: 38879781 -
Toxicol Appl Pharmacol
Paeoniflorin attenuates hyperprolactinemia by targeting the pituitary mPRα-mediated, dopamine receptor-independent signaling in vivo and in vitro. [Abstract]2025 Sep 10:505:117551. PMID: 40939721 -
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Solvent & Solubility
DMSO : 20 mg/mL (64.01 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 (protect from light). 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 (protect from light). 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)
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 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
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Data Sheet (287 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [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 (protect from light). 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 | 3.2006 mL | 16.0030 mL | 32.0059 mL | 80.0149 mL |
| 5 mM | 0.6401 mL | 3.2006 mL | 6.4012 mL | 16.0030 mL | |
| 10 mM | 0.3201 mL | 1.6003 mL | 3.2006 mL | 8.0015 mL | |
| 15 mM | 0.2134 mL | 1.0669 mL | 2.1337 mL | 5.3343 mL | |
| 20 mM | 0.1600 mL | 0.8001 mL | 1.6003 mL | 4.0007 mL | |
| 25 mM | 0.1280 mL | 0.6401 mL | 1.2802 mL | 3.2006 mL | |
| 30 mM | 0.1067 mL | 0.5334 mL | 1.0669 mL | 2.6672 mL | |
| 40 mM | 0.0800 mL | 0.4001 mL | 0.8001 mL | 2.0004 mL | |
| 50 mM | 0.0640 mL | 0.3201 mL | 0.6401 mL | 1.6003 mL | |
| 60 mM | 0.0533 mL | 0.2667 mL | 0.5334 mL | 1.3336 mL |