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Olanzapine 5-HT Receptor antagonist

Name: Olanzapine
Brand: Selleck Chemicals
SKU: S2493
Availability: InStock
Rating: 5 (16 reviews)

Cat.No.S2493

Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

Chemical Structure

Molecular Weight: 312.43975

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Chemical Information, Storage & Stability

Molecular Weight	312.43975	Formula	C₁₇H₂₀N₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	132539-06-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera			Smiles	CC1=CC2=C(S1)NC3=CC=CC=C3N=C2N4CCN(CC4)C

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (198.43 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (4.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an 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 the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-HT2 ^[1] D2 receptor ^[1]
In vitro	Olanzapine interacts with key receptors of interest in schizophrenia, having a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors. This compound has a receptor profile that is similar to that of clozapine: it is relatively nonselective at dopamine receptor subtypes and it shows selectivity for mesolimbic and mesocortical over striatal dopamine tracts (electrophysiology; Fos). ^[1]
In vivo	Olanzapine is a potent antagonist at DA receptors (DOPAC levels; pergolide-stimulated increases in plasma corticosterone) and 5-HT receptors (quipazine-stimulated increases in corticosterone), but is weaker at alpha-adrenergic and muscarinic receptors. ^[1] This compound combined with fluoxetine produces robust, sustained increases of extracellular levels of dopamine ([DA](ex)) and norepinephrine ([NE](ex)) up to 361% and 272% of the baseline in rat prefrontal cortex, respectively, which are significantly greater than either drug alone. ^[2] It at 0.5 mg/kg, 3 mg/kg and 10 mg/kg (s.c.) dose-dependently increases the extracellular dopamine (DA) and norepinephrine (NE) levels in rat prefrontal cortex, nucleus accumbens and striatum. This chemical also increases extracellular levels of a DA metabolite, DOPAC, and tissue concentrations of a released DA metabolite, 3-methoxytyramine. ^[3] It results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. ^[4] This agent results in substantial increases in adiposity: increased total body fat reflecting marked increases in subcutaneous and visceral adipose stores. It results in marked hepatic insulin resistance. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9265914/ [2] https://pubmed.ncbi.nlm.nih.gov/10942849/ [3] https://pubmed.ncbi.nlm.nih.gov/9551772/ [4] https://pubmed.ncbi.nlm.nih.gov/15756305/ [5] https://pubmed.ncbi.nlm.nih.gov/15734866/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06288854	Not yet recruiting	Weight Gain	Rajavithi Hospital	April 3 2024	Not Applicable
NCT06319170	Recruiting	Schizophrenia Schizoaffective Disorder	Teva Branded Pharmaceutical Products R&D Inc.	March 28 2024	Phase 1
NCT06315283	Recruiting	Schizophrenia	Teva Branded Pharmaceutical Products R&D Inc.	March 20 2024	Phase 1
NCT06253546	Recruiting	Schizophrenia	Teva Branded Pharmaceutical Products R&D Inc.	March 28 2024	Phase 1

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