Granisetron | CAS# 109889-09-0 | Serotonin Receptor Antagonist

MedKoo Cat#: 574959 | Name: Granisetron

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Description:

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

Granisetron is a serotonin receptor (5HT-3 selective) antagonist that has been used as an anti-emetic for cancer chemotherapy patients.

Chemical Structure

Granisetron

CAS#109889-09-0 (free base),

Theoretical Analysis

MedKoo Cat#: 574959

Name: Granisetron

CAS#: 109889-09-0 (free base),

Chemical Formula: C18H24N4O

Exact Mass: 312.1950

Molecular Weight: 312.42

Elemental Analysis: C, 69.20; H, 7.74; N, 17.93; O, 5.12

Price and Availability

Size	Price	Availability	Quantity
50mg	USD 300.00	2 Weeks
100mg	USD 550.00	2 Weeks

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Related CAS #

107007-99-8 (HCl) 109889-09-0 (free base)

Synonym

Granisetron; APF530; APF-530; APF 530; Kevatril; Sancuso; Sustol

IUPAC/Chemical Name

1-Methyl-N-(9-methyl-endo-9-azabicyclo(3.3.1)non-3-yl)-1H-indazole-3-carboxamide

InChi Key

MFWNKCLOYSRHCJ-BTTYYORXSA-N

InChi Code

InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)

SMILES Code

O=C(C1=NN(C)C2=C1C=CC=C2)NC3CC(N4C)CCCC4C3

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

Shelf Life

>3 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:

Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist.

In vitro activity:

In another separate experiment, granisetron effect on neuronal Ca+2 flux induced by Aβ42 (2 μM) acute exposure was also evaluated. Granisetron significantly reduced Aβ42-induced Ca+2 flux by ~40% (Fig. 3D). Reference: J Alzheimers Dis. 2019;72(4):1097-1117. https://pubmed.ncbi.nlm.nih.gov/31683487/

In vivo activity:

Granisetron significantly reduced the serum levels of ALT, AST, and bilirubin in CLP-induced rat liver injury by 41.96%, 59.61%, and 45.16% (p < 0.05), respectively when compared with the CLP-group. Regarding serum albumin, granisetron significantly increased the level of albumin by 253.38% (p < 0.05) as compared with the CLP-group (Table 2). Reference: J Pharmacol Sci. 2021 Dec;147(4):358-366. https://pubmed.ncbi.nlm.nih.gov/34663518/

	Solvent	mg/mL	mM
Solubility
	DMSO	11.0	35.21

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 312.42 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. Al Rihani SB, Lan RS, Kaddoumi A. Granisetron Alleviates Alzheimer's Disease Pathology in TgSwDI Mice Through Calmodulin-Dependent Protein Kinase II/cAMP-Response Element Binding Protein Pathway. J Alzheimers Dis. 2019;72(4):1097-1117. doi: 10.3233/JAD-190849. PMID: 31683487; PMCID: PMC7183768. 2. Wang J, Gong S, Wang F, Niu M, Wei G, He Z, Gu T, Jiang Y, Liu A, Chen P. Granisetron protects polymicrobial sepsis-induced acute lung injury in mice. Biochem Biophys Res Commun. 2019 Jan 22;508(4):1004-1010. doi: 10.1016/j.bbrc.2018.12.031. Epub 2018 Dec 11. PMID: 30551881. 3. Aboyoussef AM, Mohammad MK, Abo-Saif AA, Messiha BAS. Granisetron attenuates liver injury and inflammation in a rat model of cecal ligation and puncture-induced sepsis. J Pharmacol Sci. 2021 Dec;147(4):358-366. doi: 10.1016/j.jphs.2021.08.005. Epub 2021 Sep 4. PMID: 34663518.

In vitro protocol:

In vivo protocol:

1. Aboyoussef AM, Mohammad MK, Abo-Saif AA, Messiha BAS. Granisetron attenuates liver injury and inflammation in a rat model of cecal ligation and puncture-induced sepsis. J Pharmacol Sci. 2021 Dec;147(4):358-366. doi: 10.1016/j.jphs.2021.08.005. Epub 2021 Sep 4. PMID: 34663518. 2. Al Rihani SB, Lan RS, Kaddoumi A. Granisetron Alleviates Alzheimer's Disease Pathology in TgSwDI Mice Through Calmodulin-Dependent Protein Kinase II/cAMP-Response Element Binding Protein Pathway. J Alzheimers Dis. 2019;72(4):1097-1117. doi: 10.3233/JAD-190849. PMID: 31683487; PMCID: PMC7183768.

1: Wu SJ, Xiong XZ, Lin YX, Cheng NS. Comparison of the efficacy of ondansetron and granisetron to prevent postoperative nausea and vomiting after laparoscopic cholecystectomy: a systematic review and meta-analysis. Surg Laparosc Endosc Percutan Tech. 2013 Feb;23(1):79-87. doi: 10.1097/SLE.0b013e31827549e8. Review. PubMed PMID: 23386158. 2: Hsu ES. A review of granisetron, 5-hydroxytryptamine3 receptor antagonists, and other antiemetics. Am J Ther. 2010 Sep-Oct;17(5):476-86. doi: 10.1097/MJT.0b013e3181ea7821. Review. PubMed PMID: 20844345. 3: Duggan ST, Curran MP. Transdermal granisetron. Drugs. 2009;69(18):2597-605. doi: 10.2165/11202780-000000000-00000. Review. PubMed PMID: 19943709. 4: Vrabel M. Is ondansetron more effective than granisetron for chemotherapy-induced nausea and vomiting? A review of comparative trials. Clin J Oncol Nurs. 2007 Dec;11(6):809-13. Review. PubMed PMID: 18063539. 5: Feyer P, Seegenschmiedt MH, Steingraeber M. Granisetron in the control of radiotherapy-induced nausea and vomiting: a comparison with other antiemetic therapies. Support Care Cancer. 2005 Sep;13(9):671-8. Epub 2005 Jul 26. Review. PubMed PMID: 16044252.