Tegaserod maleate 马来酸替加色罗; SDZ-HTF-919; HTF-919|cas:189188-57-6|西域试剂

Tegaserod maleate 马来酸替加色罗; SDZ-HTF-919; HTF-919,99.93%

产品编号：Bellancom-14153A| CAS NO：189188-57-6| 分子式：C₂₀H₂₇N₅O₅| 分子量：417.46

Tegaserod马来酸盐是5-HT4激动剂。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-14153A		￥920.00	杭州北京（现货）
Bellancom-14153A		￥2900.00	杭州北京（现货）

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Tegaserod maleate 马来酸替加色罗; SDZ-HTF-919; HTF-919

产品介绍

Tegaserod maleate (SDZ-HTF-919) 是一种口服有效的 5-羟色胺受体 4 (HTR4; 5-HT₄R) 激动剂和 5-HT_2B 受体拮抗剂。Tegaserod maleate 对人重组 5-HT_2A、5-HT_2B 和 5-HT_2C 受体的 pK_is 分别为 7.5、8.4 和 7.0。Tegaserod maleate 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 maleate 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。

生物活性

Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod maleate has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C 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-HT_2B 受体拮抗剂活性一致。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	A375, RPMI-7951 (RPMI), SH4, B16F10, MeWo and MEL-JUSO
Concentration:	3, 5 μM
Incubation Time:	24, 48, 72 h
Result:	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.

体内研究
(In Vivo)

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% .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 35 mg/mL (83.84 mM)

H₂O : 1 mg/mL (2.40 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3954 mL	11.9772 mL	23.9544 mL
5 mM	0.4791 mL	2.3954 mL	4.7909 mL
10 mM	0.2395 mL	1.1977 mL	2.3954 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

. 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]

. 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]

. 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]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

危险品运输编码	NONH for all modes of transport
海关编码	2933990090

1. 物质的识别

产品名：	Tegaserod maleate
CAS号：	189188-57-6
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Tegaserod maleate
别名：	SDZ-HTF-919; HTF-919
分子式：	C20H27N5O5
分子量：	417.46

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

110-16-7

145158-71-0

~72%

189188-57-6

文献：Venkataraman, Sundaram; Gudipati, Srinivasulu; Mandava Venkata Naga, Brahmeshwararao; Banda, Goverdhan Reddy; Singamsetty, Radhakrishna Patent: US2005/272802 A1, 2005 ; Location in patent: Page/Page column 2-3 ;

上游产品 2
110-16-7 145158-71-0
下游产品 0

[1]. Bushman J, et al. Tegaserod mimics the neurostimulatory glycan polysialic acid and promotes nervous system repair. Neuropharmacology. 2014 Apr;79:456-66.

[2]. Yan C, et al. Effect of the 5-HT4 receptor and serotonin transporter on visceral hypersensitivity in rats. Braz J Med Biol Res. 2012 Oct;45(10):948-54.

[3]. Painsipp E, et al. Alosetron, cilansetron and tegaserod modify mesenteric but not colonic blood flow in rats. Br J Pharmacol. 2009 Nov;158(5):1210-26.

Tegaserod maleate 马来酸替加色罗; SDZ-HTF-919; HTF-919,99.93%

Tegaserod maleate 马来酸替加色罗; SDZ-HTF-919; HTF-919

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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