产品
编 号：F236662
分子式：C20H27N5O5
分子量：417.46
分子式：C20H27N5O5
分子量：417.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 189188-57-6
产品详情
生物活性：
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
体内研究：
马来酸替加色罗 (SDZ-HTF-919; 5 mg/kg/天; 腹腔注射; 连续五天) 在体内延迟肿瘤生长、减少转移、增加存活率并抑制 p-S6。马来酸替加色罗 (0.1-2.0 mg/kg; 胃负荷前 15 分钟腹腔注射) 显着加速 db/db 小鼠的胃葡萄糖排空率，在 0.1mg/kg 的情况下将 30 分钟时留在胃中的膳食部分减少 80% .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 mice
Dosage: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).
体外研究：
马来酸替加色罗 (SDZ-HTF-919; 3-5 μM; 24-72 小时) 引起显着的时间和剂量依赖性细胞凋亡增加。马来酸替加色罗 (3-5 μM; 8-18 小时) 降低 p-S6 ，p-p70 S6 (Thr421/Ser424)。马来酸替加色罗 (0.1-3 μM; 24 小时) 有效抑制 5-HT 介导的大鼠离体胃底收缩 (pA2=8.3)，与 5-HT2B 受体拮抗剂活性一致。
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
体内研究：
马来酸替加色罗 (SDZ-HTF-919; 5 mg/kg/天; 腹腔注射; 连续五天) 在体内延迟肿瘤生长、减少转移、增加存活率并抑制 p-S6。马来酸替加色罗 (0.1-2.0 mg/kg; 胃负荷前 15 分钟腹腔注射) 显着加速 db/db 小鼠的胃葡萄糖排空率，在 0.1mg/kg 的情况下将 30 分钟时留在胃中的膳食部分减少 80% .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 mice
Dosage: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).
体外研究：
马来酸替加色罗 (SDZ-HTF-919; 3-5 μM; 24-72 小时) 引起显着的时间和剂量依赖性细胞凋亡增加。马来酸替加色罗 (3-5 μM; 8-18 小时) 降低 p-S6 ，p-p70 S6 (Thr421/Ser424)。马来酸替加色罗 (0.1-3 μM; 24 小时) 有效抑制 5-HT 介导的大鼠离体胃底收缩 (pA2=8.3)，与 5-HT2B 受体拮抗剂活性一致。
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