Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
Other Sizes |
|
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. 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.
Targets |
5-HT3 Receptor ( IC50 = 17 μM )
|
||
---|---|---|---|
ln Vitro |
|
||
ln Vivo |
|
||
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 |
|
||
References |
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
|
Related CAS # |
Granisetron; 109889-09-0
|
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.77 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.77 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 100 mg/mL (286.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
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 |
![]() |
---|
![]() |
![]() |