Dalasetron Mesylate - CAS 115956-13-3
Catalog number:
115956-13-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H27N2O7S
Molecular Weight:
439.50
COA:
Inquire
Targets:
5-HT Receptor
Description:
The mesylate salt form of Dolasetron which is a pseudopelletierine derivative and could be used to relieve the nausea and vomiting caused by chemotherapy for behaving as a 5-HT3 receptor antagonist.
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Purity:
98.0%~102.0%
Appearance:
Powder
Synonyms:
MDL-73147EF; Anzemet; Anemet; NCGC00181048-01; Dolasetron mesilate
Solubility:
10 mM in DMSO
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
The mesylate salt form of Dolasetron could be used to relieve the nausea and vomiting caused by chemotherapy for behaving as a 5-HT3 receptor antagonist.
Quality Standard:
USP
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Grams-Kilos
InChIKey:
QTFFGPOXNNGTGZ-RCSCTSIBSA-N
InChI:
InChI=1S/C19H20N2O3.CH4O3S.H2O/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17;1-5(2,3)4;/h1-4,9,11-14,20H,5-8,10H2;1H3,(H,2,3,4);1H2/t11?,12-,13+,14?;
Canonical SMILES:
CS(=O)(=O)O.C1C2CC3CC(CC1N3CC2=O)OC(=O)C4=CNC5=CC=CC=C54.O
1.Results from the IQ-CSRC prospective study support replacement of the thorough QT study by QT assessment in the early clinical phase.
Darpo B1, Benson C, Dota C, Ferber G, Garnett C, Green CL, Jarugula V, Johannesen L, Keirns J, Krudys K, Liu J, Ortemann-Renon C, Riley S, Sarapa N, Smith B, Stoltz RR, Zhou M, Stockbridge N. Clin Pharmacol Ther. 2015 Apr;97(4):326-35. doi: 10.1002/cpt.60.
The QT effects of five "QT-positive" and one negative drug were tested to evaluate whether exposure-response analysis can detect QT effects in a small study with healthy subjects. Each drug was given to nine subjects (six for placebo) in two dose levels; positive drugs were chosen to cause 10 to 12 ms and 15 to 20 ms QTcF prolongation. The slope of the concentration/ΔQTc effect was significantly positive for ondansetron, quinine, dolasetron, moxifloxacin, and dofetilide. For the lower dose, an effect above 10 ms could not be excluded, i.e., the upper bound of the confidence interval for the predicted mean ΔΔQTcF effect was above 10 ms. For the negative drug, levocetirizine, a ΔΔQTcF effect above 10 ms was excluded at 6-fold the therapeutic dose. The study provides evidence that robust QT assessment in early-phase clinical studies can replace the thorough QT study.
2.The prospective IQ-CSRC trial: A prototype early clinical proarrhythmia assessment investigation for replacing the ICH E14 thorough QTc (TQT) study.
Cavero I1, Holzgrefe H2, Clements M3. J Pharmacol Toxicol Methods. 2016 Mar 9;80:1-8. doi: 10.1016/j.vascn.2016.02.181. [Epub ahead of print]
INTRODUCTION: Early clinical Phase I ECG investigations designed to replace the currently applied thorough QT (TQT) study are reviewed to examine how they could complement and verify the conclusions of nonclinical investigations and, in particular, the Comprehensive in vitro Proarrhythmia Assay (CiPA).
3.The modulation of carbonyl reductase 1 by polyphenols.
Boušová I1, Skálová L1, Souček P2, Matoušková P1. Drug Metab Rev. 2015;47(4):520-33. doi: 10.3109/03602532.2015.1089885. Epub 2015 Sep 29.
Carbonyl reductase 1 (CBR1), an enzyme belonging to the short-chain dehydrogenases/reductases family, has been detected in all human tissues. CBR1 catalyzes the reduction of many xenobiotics, including important drugs (e.g. anthracyclines, nabumetone, bupropion, dolasetron) and harmful carbonyls and quinones. Moreover, it participates in the metabolism of a number of endogenous compounds and it may play a role in certain pathologies. Plant polyphenols are not only present in many human food sources, but are also a component of many popular dietary supplements and herbal medicines. Many studies reviewed herein have demonstrated the potency of certain flavonoids, stilbenes and curcuminoids in the inhibition of the activity of CBR1. Interactions of these polyphenols with transcriptional factors, which regulate CBR1 expression, have also been reported in several studies. As CBR1 plays an important role in drug metabolism as well as in the protection of the organism against potentially harmful carbonyls, the modulation of its expression/activity may have significant pharmacological and/or toxicological consequences.
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Chemical Structure

CAS 115956-13-3 Dalasetron Mesylate

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