Tesofensine

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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。

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 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℃, 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].