Olanzapine (LY170053)

Alias: LY170053; LY-170052; Olanzapine; LY 170052; Zyprexa; Zolafren

Cat No.:V0963 Purity: ≥98%

COA Product Data Instructions for use SDS

Olanzapine (LY170053) Chemical Structure CAS No.: 132539-06-1
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

Size	Price	Stock	Qty
500mg
1g
2g
5g
10g
Other Sizes

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Other Forms of Olanzapine (LY170053):

Olanzapine D3

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Olanzapine (formerly LY-170052, LY 170052, Zyprexa, Zolafren), a thienobenzodiazepine analog, is an approved atypical antipsychotic drug with high affinity for 5-HT2 serotonin and D2 dopamine receptor. It functions as a 5-HT2 antagonist of dopamine and serotonin. According to binding studies, olanzapine exhibited a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors, and interacted with key receptors of interest in schizophrenia. The U.S. FDA has approved it for the treatment of bipolar disorder and schizophrenia. Olanzapine and quetiapine share structural similarities.

Biological Activity I Assay Protocols (From Reference)

Targets

5-HT_2A Receptor ( Ki = 4 nM ); 5-HT₁ Receptor ( Ki = 7 nM ); 5-HT₆ Receptor ( Ki = 5 nM ); 5-HT_2C Receptor ( Ki = 11 nM ); 5-HT₃ Receptor ( Ki = 57 nM ); Adrenergic α1 Receptor ( Ki = 19 nM ); Muscarinic M1-5 Receptor ( Ki = 1.9-25 nM ); Dopamine Receptor; Mitophagy; Apoptosis

ln Vitro

In vitro activity: Olanzapine has a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors, which allows it to interact with important receptors implicated in schizophrenia. Similar to clozapine, olanzapine exhibits a receptor profile that is largely nonselective at dopamine receptor subtypes, with selectivity for mesolimbic and mesocortical dopamine tracts over striatal dopamine tracts (electrophysiology; Fos). [1]

ln Vivo

Olanzapine is a weaker antagonist at alpha-adrenergic and muscarinic receptors, but a strong antagonist at DA receptors (DOPAC levels; pergolide-stimulated increases in plasma corticosterone) and 5-HT receptors (quipazine-stimulated increases in corticosterone).[1] In the rat prefrontal cortex, olanzapine plus fluoxetine together result in strong, prolonged increases in extracellular levels of norepinephrine ([NE](ex)) and dopamine ([DA](ex)) up to 361% and 272% of the baseline, respectively. These increases are noticeably higher than those caused by either medication alone.[2] In rat prefrontal cortex, nucleus accumbens, and striatum, olanzapine at 0.5 mg/kg, 3 mg/kg, and 10 mg/kg (s.c.) dose-dependently raises the extracellular dopamine (DA) and norepinephrine (NE) levels. Olanzapine also raises the concentrations of 3-methoxytyramine, a released DA metabolite, in tissues and extracellular levels of DOPAC, another DA metabolite.[3] Fresh brain weights on average and left cerebrum volumes and fresh weights in macaque monkeys are reduced by 8–11% when olanzapine is administered. [4] Obesity is significantly elevated when taking olanzapine; elevated visceral and subcutaneous adipose stores are reflected in elevated total body fat. Hepatic insulin resistance is brought on by olanzapine.[5]

Animal Protocol

0.5 mg/kg, 3 mg/kg and 10 mg/kg (s.c.)

Macaque monkeys

References

[1]. J Clin Psychiatry . 1997:58 Suppl 10:28-36.

[2]. Neuropsychopharmacology . 2000 Sep;23(3):250-62

[3]. Psychopharmacology (Berl) . 1998 Mar;136(2):153-61.

[4]. Neuropsychopharmacology . 2005 Sep;30(9):1649-61.

[5]. Diabetes . 2005 Mar;54(3):862-71.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C17H20N4S

Molecular Weight

312.44

Exact Mass

312.14

Elemental Analysis

C, 65.35; H, 6.45; N, 17.93; S, 10.26

CAS #

132539-06-1

Related CAS #

Olanzapine-d3; 786686-79-1

Appearance

Solid powder

SMILES

CC1=CC2=C(S1)NC3=CC=CC=C3N=C2N4CCN(CC4)C

InChi Key

KVWDHTXUZHCGIO-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,19H,7-10H2,1-2H3

Chemical Name

2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine

Synonyms

LY170053; LY-170052; Olanzapine; LY 170052; Zyprexa; Zolafren

HS Tariff Code

2934.99.9001

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)

Solubility Data

Solubility (In Vitro)

DMSO: 20~63 mg/mL (64.0~201.6 mM)

Water: <1 mg/mL

Ethanol: ~9 mg/mL (~28.8 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.2006 mL	16.0031 mL	32.0061 mL
	5 mM	0.6401 mL	3.2006 mL	6.4012 mL
	10 mM	0.3201 mL	1.6003 mL	3.2006 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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02088060	Active Recruiting	Drug: Cannabidiol Drug: Olanzapine	Schizophrenia	Central Institute of Mental Health, Mannheim	December 8, 2015	Phase 2
NCT05213143	Active Recruiting	Drug: Lurasidone	Schizophrenia	Sumitomo Pharma (Suzhou) Co., Ltd.	December 30, 2021	Phase 4
NCT00512070	Active Recruiting	Drug: olanzapine and melatonin	Schizophrenia Obesity	Seattle Institute for Biomedical and Clinical Research	July 2007	Not Applicable
NCT05244577	Recruiting	Drug: Olanzapine Tablets Drug: Placebo	Olanzapine CINV Cisplatin	Shi Yanxia	January 18, 2022	Phase 3
NCT05243251	Recruiting	Drug: Olanzapine 5 MG Drug: Placebo	Anorexia	Cairo University	December 25, 2021	Phase 3

Biological Data

Effects of olanzapine (3 mg/kg, s.c.) and fluoxetine (10 mg/kg, s.c.) alone and in combination on [5-HT]ex (A), [DA]ex (B), and [NE]ex (C) in the rat prefrontal cortex. Neuropsychopharmacology . 2000 Sep;23(3):250-62.

Effects of olanzapine (3 mg/kg, s.c.) and sertraline (10 mg/kg, s.c.) alone and in combination on [5-HT]ex (A), [DA]ex (B), and [NE]ex (C) in the rat prefrontal cortex. Neuropsychopharmacology . 2000 Sep;23(3):250-62.

Administrated daily drug dose as a function of time for each monkey in the haloperidol- (left) and olanzapine- (right) exposed groups. Neuropsychopharmacology . 2005 Sep;30(9):1649-61.
Increase in mean body weights for each group (S, sham; H, haloperidol; O, olanzapine) across the course of the study. Neuropsychopharmacology . 2005 Sep;30(9):1649-61.
Fresh brain weights for the sham- (S), haloperidol- (H) and olanzapine- (O) exposed monkeys. Neuropsychopharmacology . 2005 Sep;30(9):1649-61.