Granisetron HCl (BRL 43694A)

Alias: BRL43694; BRL 43694; BRL43694A; BRL 43694A; BRL-43694; BRL-43694A; Granisetron Hydrochloride; Granisetron HCl; GRAN; US trade name: Kytril
Cat No.:V0976 Purity: ≥98%
Granisetron HCl (BRL-43694; BRL43694; BRL-43694A; trade name: Kytril), an approved antiemetic drug, is a potent serotonin 5-HT3 receptor antagonist with antiemetic activity.
Granisetron HCl (BRL 43694A) Chemical Structure CAS No.: 107007-99-8
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
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1g
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Other Forms of Granisetron HCl (BRL 43694A):

  • Granisetron
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Granisetron HCl (BRL-43694; BRL43694; BRL-43694A; trade name: Kytril), an approved antiemetic drug, is a potent serotonin 5-HT3 receptor antagonist with antiemetic activity. It is used to treat nausea and vomiting brought on by chemotherapy. Granisetron, with a KD of 4.3 mM, inhibits the delayed rectifier current (IK) of isolated feline ventricular myocytes. Granisetron exhibits an inherent voltage dependence as depolarization causes the block to increase. Granisetron blocks are deposited at a binding site 10% across the transmembrane electrical field from the intracellular side. In feline isolated ventricular myocytes, granisetron (3 mM) prolongs the action potential duration (APD) by approximately 30% at 0.5 Hz.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT3 Receptor ( IC50 = 17 μM )
ln Vitro

In vitro activity: Granisetron inhibits feline isolated ventricular myocytes' delayed rectifier current (IK) at a 4.3 mM KD. Granisetron exhibits an inherent voltage dependence when the depolarization increases the block. At a binding site 10% across the transmembrane electrical field, granisetron blocks are inserted from the intracellular side. The action potential duration (APD) in feline isolated ventricular myocytes is prolonged by approximately 30% at 0.5 Hz by granisetron (3 mM).[1] Granisetron, but not Ondansetron, has the ability to stop potential 5-H autoreceptors from activating, which would reduce the amount of serotonin released by enterochromaffin cells.[2]

ln Vivo
Granisetron significantly reduces the risk of cisplatin-induced emesis in piglets; certain animals are fully protected against both the acute and delayed phases of the condition.[2] When given three times a day, granisetron (1 mg/kg, i.m.) dramatically lessens the vomiting and retching that cats experience on days 1 and 2 as a result of cisplatin by 100% and 75%, respectively.[3] In rats, granisetron or dexamethasone significantly reduces colonic levels of malondialdehyde and inflammatory cytokines, inhibits myeloperoxidase activity, and improves macroscopic and histologic scores.[4] Granisetron, not only prevents cholera toxin-induced jejunal net fluid secretion but also, and in proportion, inhibits 5-HT release into the intestinal lumen of mice.[5]
Cell Assay
In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. GR 0.003-0.03 nM dose-dependently decreased s-HT tachycardia in the isolated rabbit heart; at high concentrations, GR decreased both submaximal and maximal responses to 5-HT.
Animal Protocol
1 mg/kg, i.m.
Piglet
References

[1]. Br J Pharmacol . 1994 Oct;113(2):527-35.

[2]. J Pharmacol Exp Ther . 1996 Oct;279(1):255-61.

[3]. Eur J Pharmacol . 2000 Mar 10;391(1-2):145-50.

[4]. Hum Exp Toxicol . 2010 Apr;29(4):321-8.

[5]. Br J Pharmacol . 2000 Jul;130(5):1031-6.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H25CLN4O
Molecular Weight
348.87
Exact Mass
312.2
Elemental Analysis
C, 61.97; H, 7.22; Cl, 10.16; N, 16.06; O, 4.59
CAS #
107007-99-8
Appearance
White solid powder
SMILES
CN1C2CCCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C.Cl
InChi Key
QYZRTBKYBJRGJB-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H24N4O.ClH/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);1H
Chemical Name
1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)indazole-3-carboxamide;hydrochloride
Synonyms
BRL43694; BRL 43694; BRL43694A; BRL 43694A; BRL-43694; BRL-43694A; Granisetron Hydrochloride; Granisetron HCl; GRAN; US trade name: Kytril
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: 7.7~70 mg/mL (22.0~200.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8664 mL 14.3320 mL 28.6640 mL
5 mM 0.5733 mL 2.8664 mL 5.7328 mL
10 mM 0.2866 mL 1.4332 mL 2.8664 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.

(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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05325190 Recruiting Drug: Granisetron Transdermal
Patch System
Chemotherapy-induced Nausea
and Vomiting
Tianjin Medical University Cancer
Institute and Hospital
October 10, 2021 Phase 2
NCT04472143 Recruiting Drug: Granisetron Transdermal
Other: 0.9% normal saline
Granisetron Assiut University April 2022 Phase 2
Phase 3
NCT05314257 Recruiting Drug: Granisetron Hydrochloride
Behavioral: Resistance training
Histamine University Ghent September 1, 2023 Not Applicable
NCT03817970 Recruiting Drug: Granisetron
Drug: Ondansetron
Drug: Palonosetron
Nephrotoxicity University of Colorado, Denver November 15, 2019 Phase 3
NCT00873197 Completed Drug: granisetron Healthy Prostrakan Pharmaceuticals April 2009 Phase 1
Biological Data
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