Size | Price | Stock | Qty |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
GR exhibited an IC50 of 17/± 6 uM in rat forestomach, reducing 5-HT-induced contractions. GR decreased s-HT tachycardia in isolated rabbit hearts in a dose-dependent manner with a range of 0.003-0.03 nM; high GR levels also decreased submaximal and maximum responses to 5-HT [1].
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ln Vivo |
Six and 72 hours after the development of inflammation, granisetron dose-dependently reduced leukocyte accumulation. PGE(2) levels were elevated by Granisetron at lower dosages (50 μg/bag), but release was suppressed at higher doses (100 and 200 μg/bag). Concurrently, granisetron at lower doses will decrease TNFα production, but granisetron at higher doses will enhance TNFα production; these two effects are reciprocal [2]. It was demonstrated that GTDS was not inferior to oral granisetron: 65% of patients receiving oral granisetron and 60% of patients receiving GTDS obtained complete control (treatment difference, -5%; 95% confidence range, -13-3). Constipation was the most frequent side effect of both well-tolerated therapies [3].
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References |
[1]. Sanger GJ, Nelson DR. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113-24.
[2]. Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6. [3]. Boccia RV, Gordan LN, Clark G, Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III |
Molecular Formula |
C18H24N4O
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Molecular Weight |
312.40936
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CAS # |
109889-09-0
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Related CAS # |
Granisetron Hydrochloride;107007-99-8;Granisetron-d3;1224925-64-7
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SMILES |
CN1N=C(C(N[C@H]2C[C@H](N3C)CCC[C@H]3C2)=O)C4=CC=CC=C41
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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)
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Solubility (In Vitro) |
DMSO : ~25 mg/mL (~80.02 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.00 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 25.0 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: ≥ 2.5 mg/mL (8.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2009 mL | 16.0046 mL | 32.0092 mL | |
5 mM | 0.6402 mL | 3.2009 mL | 6.4018 mL | |
10 mM | 0.3201 mL | 1.6005 mL | 3.2009 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.