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Tesofensine
本半岛bd体育手机客户端 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

半岛bd体育手机客户端 名称
NS-2330
半岛bd体育手机客户端 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 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 --- --- ---
*

请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 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].
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