Granisetron-d3
Based on 1 Customer Validation
Granisetron-d3 is the deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
For research use only. We do not sell to patients.
- CAS No.: 1224925-64-7
- Formula: C18H21D3N4O
- Molecular Weight:315.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.32 μM
Compound: Granisetron, Kutril
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Agonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells by FLIPR assay
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[PMID: 24128813] |
| HEK293 | EC50 |
0.5 μM
Compound: Granisetron, Kutril
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Agonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells by FLIPR assay
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[PMID: 24128813] |
| HEK293 | IC50 |
311 μM
Compound: granisetron
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Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
4.3 μM
Compound: granisetron
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Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
5 μM
Compound: granisetron
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1224925-64-7
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Unlabeled Cas 109889-09-0
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Molecular Weight 315.43
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Formula C18H21D3N4O
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SMILES
C(N[C@H]1C[C@@H]2N(C([2H])([2H])[2H])[C@H](C1)CCC2)(=O)C=3C=4C(N(C)N3)=CC=CC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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 study. Support Care Cancer. 2011 Oct;19(10):1609-17. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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