Olanzapine | CAS#132539-06-1 | LY-170052

MedKoo Cat#: 318383 | Name: Olanzapine

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Olanzapine is an atypical antipsychotic. It is approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia and bipolar disorder. Olanzapine is structurally similar to clozapine and quetiapine. It is a dopamine antagonist and is classified as a thienobenzodiazepine.

Chemical Structure

Olanzapine

CAS#132539-06-1 (free base)

Theoretical Analysis

MedKoo Cat#: 318383

Name: Olanzapine

CAS#: 132539-06-1 (free base)

Chemical Formula: C17H20N4S

Exact Mass: 312.1409

Molecular Weight: 312.43

Elemental Analysis: C, 65.35; H, 6.45; N, 17.93; S, 10.26

Price and Availability

Size	Price	Availability	Quantity
1g	USD 350.00
2g	USD 550.00
5g	USD 950.00

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Related CAS #

132539-06-1 (free base); 783334-36-1 (HCl)

Synonym

LY-170052, LY170052, LY 170052, Olanzapine, Zyprexa, Zolafren

IUPAC/Chemical Name

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

InChi Key

WXPNDRBBWZMPQG-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/h3-6,11,18H,7-10H2,1-2H3

SMILES Code

CN1CCN(C2=C(C=C(C)S3)C3=NC4=CC=CC=C4N2)CC1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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).

In vitro activity:

This study’s initial hypothesis that olanzapine may enhance temozolomide's anti-tumor activity could be confirmed in U87MG and A172 glioblastoma cell lines. Moreover, treatment with olanzapine alone resulted in a marked anti-proliferative effect on U87MG, A172 and two glioma stem-like cells with IC50 values ranging from 25 to 79.9 µM. In U87MG cells, anchorage-independent growth was dose-dependently inhibited. Reference: J Neurooncol. 2015 Mar;122(1):21-33. https://pubmed.ncbi.nlm.nih.gov/25524815/

In vivo activity:

In experiment 1, the highest dose of chronically administered olanzapine (3 mg/kg) induced significant weight gain accompanied by augmentation of periuterine fat depots, with no changes in locomotor activity. In experiment 2, chronic administration did not alter energy expenditure, whereas, decreased respiratory quotient (RQ). In experiment 3, subcutaneously infused olanzapine evidenced a dose and time-dependent increase of body weight and HF-HS diet consumed. Reference: Psychopharmacology (Berl). 2006 Jul;186(4):561-71. https://pubmed.ncbi.nlm.nih.gov/16758241/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	64.01
	DMSO	32.3	103.41
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.60
	Ethanol	8.0	25.61

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 312.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Vucicevic L, Misirkic-Marjanovic M, Paunovic V, Kravic-Stevovic T, Martinovic T, Ciric D, Maric N, Petricevic S, Harhaji-Trajkovic L, Bumbasirevic V, Trajkovic V. Autophagy inhibition uncovers the neurotoxic action of the antipsychotic drug olanzapine. Autophagy. 2014;10(12):2362-78. doi: 10.4161/15548627.2014.984270. PMID: 25551567; PMCID: PMC4502661. 2. Karpel-Massler G, Kast RE, Westhoff MA, Dwucet A, Welscher N, Nonnenmacher L, Hlavac M, Siegelin MD, Wirtz CR, Debatin KM, Halatsch ME. 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. doi: 10.1007/s11060-014-1688-7. Epub 2014 Dec 19. PMID: 25524815. 3. Liu X, Zhang H, Zhang S, Mao W, Liu L, Deng C, Hu CH. Olanzapine-induced decreases of FGF21 in brown adipose tissue via histone modulations drive UCP1-dependent thermogenetic impairment. Prog Neuropsychopharmacol Biol Psychiatry. 2023 Mar 2;122:110692. doi: 10.1016/j.pnpbp.2022.110692. Epub 2022 Dec 9. PMID: 36509252. 4. Coccurello R, Caprioli A, Ghirardi O, Conti R, Ciani B, Daniele S, Bartolomucci A, Moles A. Chronic administration of olanzapine induces metabolic and food intake alterations: a mouse model of the atypical antipsychotic-associated adverse effects. Psychopharmacology (Berl). 2006 Jul;186(4):561-71. doi: 10.1007/s00213-006-0368-5. Epub 2006 May 13. PMID: 16758241.

In vitro protocol:

In vivo protocol:

1. Liu X, Zhang H, Zhang S, Mao W, Liu L, Deng C, Hu CH. Olanzapine-induced decreases of FGF21 in brown adipose tissue via histone modulations drive UCP1-dependent thermogenetic impairment. Prog Neuropsychopharmacol Biol Psychiatry. 2023 Mar 2;122:110692. doi: 10.1016/j.pnpbp.2022.110692. Epub 2022 Dec 9. PMID: 36509252. 2. Coccurello R, Caprioli A, Ghirardi O, Conti R, Ciani B, Daniele S, Bartolomucci A, Moles A. Chronic administration of olanzapine induces metabolic and food intake alterations: a mouse model of the atypical antipsychotic-associated adverse effects. Psychopharmacology (Berl). 2006 Jul;186(4):561-71. doi: 10.1007/s00213-006-0368-5. Epub 2006 May 13. PMID: 16758241.

1: Fonte C, Fatigoni S, Roila F. A review of olanzapine as an antiemetic in chemotherapy-induced nausea and vomiting and in palliative care patients. Crit Rev Oncol Hematol. 2015 Aug;95(2):214-21. doi: 10.1016/j.critrevonc.2015.02.010. Epub 2015 Mar 5. Review. PubMed PMID: 25779971. 2: Ennis ZN, Damkier P. Pregnancy exposure to olanzapine, quetiapine, risperidone, aripiprazole and risk of congenital malformations. A systematic review. Basic Clin Pharmacol Toxicol. 2015 Apr;116(4):315-20. doi: 10.1111/bcpt.12372. Epub 2015 Jan 28. Review. PubMed PMID: 25536446. 3: Choi YJ. Efficacy of adjunctive treatments added to olanzapine or clozapine for weight control in patients with schizophrenia: a systematic review and meta-analysis. ScientificWorldJournal. 2015;2015:970730. doi: 10.1155/2015/970730. Epub 2015 Jan 13. Review. PubMed PMID: 25664341; PubMed Central PMCID: PMC4310265. 4: Luedecke D, Schöttle D, Karow A, Lambert M, Naber D. Post-injection delirium/sedation syndrome in patients treated with olanzapine pamoate: mechanism, incidence, and management. CNS Drugs. 2015 Jan;29(1):41-6. doi: 10.1007/s40263-014-0216-9. Review. PubMed PMID: 25424243. 5: Flank J, Sung L, Dvorak CC, Spettigue W, Dupuis LL. The safety of olanzapine in young children: a systematic review and meta-analysis. Drug Saf. 2014 Oct;37(10):791-804. doi: 10.1007/s40264-014-0219-y. Review. PubMed PMID: 25145624. 6: Kartashov VA, Chernova LV. [The detection of quentiapine and olanzapine in the biological objects]. Sud Med Ekspert. 2014 Sep-Oct;57(5):47-52. Review. Russian. PubMed PMID: 25764884. 7: Cristancho MA, Thase ME. Drug safety evaluation of olanzapine/fluoxetine combination. Expert Opin Drug Saf. 2014 Aug;13(8):1133-41. doi: 10.1517/14740338.2014.933804. Epub 2014 Jun 27. Review. PubMed PMID: 24972823. 8: Vella T, Mifsud J. Interactions between valproic acid and quetiapine/olanzapine in the treatment of bipolar disorder and the role of therapeutic drug monitoring. J Pharm Pharmacol. 2014 Jun;66(6):747-59. doi: 10.1111/jphp.12209. Epub 2014 Jan 7. Review. PubMed PMID: 24392714. 9: Hocking CM, Kichenadasse G. Olanzapine for chemotherapy-induced nausea and vomiting: a systematic review. Support Care Cancer. 2014 Apr;22(4):1143-51. doi: 10.1007/s00520-014-2138-y. Epub 2014 Feb 13. Review. PubMed PMID: 24522741. 10: Wang SY, Yang ZJ, Zhang L. Olanzapine for preventing nausea and vomiting induced by moderately and highly emetogenic chemotherapy. Asian Pac J Cancer Prev. 2014;15(22):9587-92. Review. PubMed PMID: 25520071. 11: Brafford MV, Glode A. Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. Review. PubMed PMID: 25032030; PubMed Central PMCID: PMC4093458. 12: Zhao J, Ou J, Xue H, Liu L, Montgomery W, Treuer T. Clinical utility of orally disintegrating olanzapine in Chinese patients with schizophrenia: a review of effectiveness, patient preference, adherence, and other properties. Neuropsychiatr Dis Treat. 2014 Feb 19;10:355-9. doi: 10.2147/NDT.S39055. eCollection 2014. Review. PubMed PMID: 24600225; PubMed Central PMCID: PMC3933704. 13: Navari RM. Olanzapine for the prevention and treatment of chronic nausea and chemotherapy-induced nausea and vomiting. Eur J Pharmacol. 2014 Jan 5;722:180-6. doi: 10.1016/j.ejphar.2013.08.048. Epub 2013 Oct 21. Review. PubMed PMID: 24157985. 14: Xue HB, Liu L, Zhang H, Montgomery W, Treuer T. Olanzapine in Chinese patients with schizophrenia or bipolar disorder: a systematic literature review. Neuropsychiatr Dis Treat. 2014 May 16;10:841-64. doi: 10.2147/NDT.S58096. eCollection 2014. Review. PubMed PMID: 24876777; PubMed Central PMCID: PMC4037301. 15: van der Zwaal EM, Janhunen SK, la Fleur SE, Adan RA. Modelling olanzapine-induced weight gain in rats. Int J Neuropsychopharmacol. 2014 Jan;17(1):169-86. doi: 10.1017/S146114571300093X. Epub 2013 Oct 8. Review. PubMed PMID: 24103788. 16: Kansagra A, Patel S, Wilcox SR. Prolonged hypothermia due to olanzapine in the setting of renal failure: a case report and review of the literature. Ther Adv Psychopharmacol. 2013 Dec;3(6):335-9. doi: 10.1177/2045125313490304. Review. PubMed PMID: 24294486; PubMed Central PMCID: PMC3840808. 17: Schöttle D, Kuhnigk O, Naber D. Drug safety evaluation of olanzapine pamoate. Expert Opin Drug Saf. 2013 Nov;12(6):897-903. doi: 10.1517/14740338.2013.832753. Epub 2013 Sep 12. Review. PubMed PMID: 24024627. 18: Lee HB, Yoon BH, Kwon YJ, Woo YS, Lee JG, Kim MD, Bahk WM. The efficacy and safety of switching to ziprasidone from olanzapine in patients with bipolar I disorder: an 8-week, multicenter, open-label study. Clin Drug Investig. 2013 Oct;33(10):743-53. doi: 10.1007/s40261-013-0120-y. Review. PubMed PMID: 23990283. 19: Schulz C, Haight RJ. Safety of olanzapine use in adolescents. Expert Opin Drug Saf. 2013 Sep;12(5):777-82. doi: 10.1517/14740338.2013.815164. Epub 2013 Jul 22. Review. PubMed PMID: 23876012. 20: Perera V, Gross AS, Polasek TM, Qin Y, Rao G, Forrest A, Xu J, McLachlan AJ. Considering CYP1A2 phenotype and genotype for optimizing the dose of olanzapine in the management of schizophrenia. Expert Opin Drug Metab Toxicol. 2013 Sep;9(9):1115-37. doi: 10.1517/17425255.2013.795540. Epub 2013 May 4. Review. PubMed PMID: 23641727.