Tesofensine NS-2330,99.35%

产品编号:Bellancom-14472| CAS NO:195875-84-4| 分子式:C17H23Cl2NO| 分子量:328.28

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-14472
2400.00 杭州 北京(现货)
Bellancom-14472
3800.00 杭州 北京(现货)
Bellancom-14472
7200.00 杭州 北京(现货)
Bellancom-14472
11500.00 杭州 北京(现货)

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Tesofensine NS-2330

产品介绍 Tesofensine (NS-2330) 是一种三元单胺再摄取抑制剂,可有效抑制神经递质多巴胺 (DA; IC50=6.5 nM)、去甲肾上腺素 (NE;IC50=1.7 nM) 和血清素 (5-HT;IC50=11 nM) 在突触间隙中的再摄取,并具有作为抗肥胖剂的潜力。Tesofensine 是一种中枢神经系统作用的抗肥胖剂。
生物活性

Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

体外研究
体内研究

Tesofensine (a single dose of 0.1-3  mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3 mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12 h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0 mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls.

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

Animal Model: Diet-induced obesity (DIO) rat
Dosage: 0.1-3 mg/kg
Administration: Administered subcutaneously (s.c.); a single dose (acute treatment)
Result: The threshold dose for inhibition of total food intake was 1.0 mg/kg.
The ED50 for inhibition of total food intake in DIO rats was estimated to be 1.3 mg/kg.
Animal Model: Diet-induced obesity (DIO) rat
Dosage: 2.0 mg/kg
Administration: Administered subcutaneously (s.c.) daily for over 16 days (chronic treatment)
Result: The average relative decrease in the body weight of tesofensine-treated DIO rats over the entire treatment period was 8.6±1.4%.
When comparing to vehicle controls, the relative weight loss with tesofensine was 13.8±1.4%.
体内研究

Tesofensine (a single dose of 0.1-3  mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3 mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12 h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0 mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls.

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

Animal Model: Diet-induced obesity (DIO) rat
Dosage: 0.1-3 mg/kg
Administration: Administered subcutaneously (s.c.); a single dose (acute treatment)
Result: The threshold dose for inhibition of total food intake was 1.0 mg/kg.
The ED50 for inhibition of total food intake in DIO rats was estimated to be 1.3 mg/kg.
Animal Model: Diet-induced obesity (DIO) rat
Dosage: 2.0 mg/kg
Administration: Administered subcutaneously (s.c.) daily for over 16 days (chronic treatment)
Result: The average relative decrease in the body weight of tesofensine-treated DIO rats over the entire treatment period was 8.6±1.4%.
When comparing to vehicle controls, the relative weight loss with tesofensine was 13.8±1.4%.
性状Solid
溶解性数据
In Vitro: 

DMSO : 2 mg/mL (6.09 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0462 mL 15.2309 mL 30.4618 mL
5 mM 0.6092 mL 3.0462 mL 6.0924 mL
10 mM --- --- ---
*

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 (protect from light)。-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:
  • 1.

    Tesofensine is dissolved in 0.9% saline solution.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献

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