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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1134188-56-9
- 分子式: C16H12D11N5O
- 分子量:312.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 1134188-56-9
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非標識Cas 145158-71-0
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分子量 312.45
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Tegaserod-d11 関連分類
HY-14153S 関連分類
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