Tegaserod-d11
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
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- No. CAS: 1134188-56-9
- Fòrmula: C16H12D11N5O
- Peso molecular:312.45
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
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].
Tegaserod (3-5 μM; 24-72 h) causes a significant time and dose-dependent increase in apoptosis[2].
Tegaserod (3-5 μM; 8-18 h) decreases phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr421/Ser424[2].
Tegaserod (0.1-3 μM; 24h) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA2=8.3), consistent with 5-HT2B receptor antagonist activity[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tegaserod (0.1-2.0 mg/kg; IP 15 min prior to gastric loading) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80% with 0.1mg/kg[3].
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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No. CAS 1134188-56-9
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Unlabeled Cas 145158-71-0
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Peso molecular 312.45
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Fòrmula C16H12D11N5O
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SMILES
N=C(NC([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])N/N=C/C1=CNC2=CC=C(OC)C=C21
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Wei Liu, et al. Repurposing the serotonin agonist Tegaserod as an anticancer agent in melanoma: molecular mechanisms and clinical implications. J Exp Clin Cancer Res. 2020 Feb 21;39(1):38. [Content Brief]
[3]. M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17(5):738-43. [Content Brief]
[4]. D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tegaserod-d11 Related Classifications
HY-14153S Related Classifications
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