1. GPCR/G Protein
    Neuronal Signaling
    Autophagy
    Apoptosis
  2. 5-HT Receptor
    Dopamine Receptor
    mAChR
    Adrenergic Receptor
    Autophagy
    Mitophagy
    Apoptosis
  3. Olanzapine

Olanzapine (Synonyms: LY170053)

Cat. No.: HY-14541 Purity: 99.89%
Handling Instructions

Olanzapine (LY170053) is a selective 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.

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Olanzapine Chemical Structure

Olanzapine Chemical Structure

CAS No. : 132539-06-1

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Description

Olanzapine (LY170053) is a selective 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-HT1 Receptor

7 nM (Ki)

5-HT2A Receptor

4 nM (Ki)

5-HT2C Receptor

11 nM (Ki)

5-HT3 Receptor

57 nM (Ki)

5-HT6 Receptor

5 nM (Ki)

Muscarinic M1-5 Receptor

1.9-25 nM (Ki)

Adrenergic α1 Receptor

19 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’s anti-tumor activity in glioblastoma cell lines[4].
Olanzapine induces apoptosis and necrosis in glioblastoma cell lines[4].

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]

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.

132539-06-1

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)

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
10 mM 0.3201 mL 1.6004 mL 3.2007 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

OlanzapineLY170053LY 170053LY-1700535-HT ReceptorDopamine ReceptormAChRAdrenergic ReceptorAutophagyMitophagyApoptosisSerotonin Receptor5-hydroxytryptamine ReceptorMuscarinic acetylcholine receptorBeta ReceptorMitochondrial Autophagy5-HT2D1D2antipsychoticanticholinergicmitochondrialdamageSH-SY5YneuronalcellInhibitorinhibitorinhibit

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