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  3. Olanzapine

Olanzapine  (Synonyms: LY170053)

Cat. No.: HY-14541 Purity: 99.83%
COA Handling Instructions

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.

Olanzapine Chemical Structure

Olanzapine Chemical Structure

CAS No. : 132539-06-1

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Olanzapine:

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Description

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[1][2].

IC50 & Target[1]

5-HT2A Receptor

4 nM (Ki)

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

 

In Vitro

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.

Cell Proliferation Assay[4]

Cell Line: U87MG and A172 glioblastoma cell lines as well as SC38 and SC40 glioma stem-like cells
Concentration: 1, 10, 100 μM
Incubation Time: 144 h; under serum starvation (1.5 % FBS) prior to performing MTT-assays
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.

Western Blot Analysis[4]

Cell Line: U87MG and A172 cells
Concentration: 10, 25, 50, and 100 μM
Incubation Time: 7 h, 24 h, 48 h, 72 h
Result: Led to a dose responsive decrease of pAMPK expression after 72 h of treatment.
In Vivo

Olanzapine (0.75, 1.5 and 3 mg/kg) evaluates body weight and periuterine fat mass, as well as insulin, non-esterified fatty acids, triglycerides, and glucose levels in mice[5]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Forty-two, 14, and 28 female CD-1 mice [5]
Dosage: 0.75, 1.5 and 3 mg/kg
Administration: Orally and chronically administered; 35 days
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.
Clinical Trial
Molecular Weight

312.43

Formula

C17H20N4S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC(C(N2CCN(C)CC2)=N3)=C(S1)NC4=C3C=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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 3.2007 mL 16.0036 mL 32.0072 mL 80.0179 mL
5 mM 0.6401 mL 3.2007 mL 6.4014 mL 16.0036 mL
10 mM 0.3201 mL 1.6004 mL 3.2007 mL 8.0018 mL
15 mM 0.2134 mL 1.0669 mL 2.1338 mL 5.3345 mL
20 mM 0.1600 mL 0.8002 mL 1.6004 mL 4.0009 mL
25 mM 0.1280 mL 0.6401 mL 1.2803 mL 3.2007 mL
30 mM 0.1067 mL 0.5335 mL 1.0669 mL 2.6673 mL
40 mM 0.0800 mL 0.4001 mL 0.8002 mL 2.0004 mL
50 mM 0.0640 mL 0.3201 mL 0.6401 mL 1.6004 mL
60 mM 0.0533 mL 0.2667 mL 0.5335 mL 1.3336 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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