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Tesofensine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tesofensine图片
CAS NO:195875-84-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
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 atriple monoamine reuptakeinhibitor 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[1]. Tesofensine is a CNS acting anti-obesity agent[2].

IC50& Target

DA/NE/5-HT[1]

体内研究
(In Vivo)

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[3].

Animal Model:Diet-induced obesity (DIO) rat[3]
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 ED50for inhibition of total food intake in DIO rats was estimated to be 1.3 mg/kg.
Animal Model:Diet-induced obesity (DIO) rat[3]
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%.
Clinical Trial
分子量

328.28

性状

Solid

Formula

C17H23Cl2NO

CAS 号

195875-84-4

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)

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 mg5 mg10 mg
1 mM3.0462 mL15.2309 mL30.4618 mL
5 mM0.6092 mL3.0462 mL6.0924 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:
  • 1.

    Tesofensine is dissolved in 0.9% saline solution[3].