Tegaserod

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tegaserod 是一种口服有效的 5-羟色胺受体 4 (HTR4; 5-HT4R) 激动剂和 5-HT2B 受体拮抗剂。Tegaserod 对人重组 5-HT2A、5-HT2B 和 5-HT2C 受体的 pKis 分别为 7.5、8.4 和 7.0。Tegaserod 导致肿瘤细胞凋亡，减弱 PI3K/Akt/mTOR 信号传导并降低 S6 磷酸化。Tegaserod 具有抗肿瘤活性，同时具有用于肠易激综合征 (IBS) 研究的潜力。

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.

Apoptosis Analysis Cell Line:A375, RPMI-7951 (RPMI), SH4, B16F10, MeWo and MEL-JUSO Concentration:3, 5 μM Incubation Time:24, 48, 72 hResult:There was a significant time and dose-dependent increase in apoptosis in all cell lines.Western Blot Analysis Cell Line:RPMI, SH4 and B16F10 cells Concentration:3, 5 μM Incubation Time:8 or 18?h Result:Decreased phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr421/Ser424.

Animal Model:C57BL/6?J mice were subcutaneously injected with B16F10 cells Dosage:5?mg/kg Administration:Administered intraperitoneally (i.p.) daily for five consecutive days Result:Treatment significantly decreased tumor growth and resulted in only slight decreases in weight following treatment.Animal Model:Female C57BLKS/J db/db miceDosage:0.1, 0.5, 1.0, 2.0 mg/kg Administration:IP 15 min prior to gastric loading Result: Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg). Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg).Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was significantly greater (2.0 mg/kg).Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg).

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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145158-71-0

301.39

C16H23N5O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (165.90 mM; 超声助溶 )

N=C(NN=CC1=CNC=2C=CC(OC)=CC12)NCCCCC

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(-20℃)

With Ice Pack

≥ 2 years