Tesofensine|195875-84-4|(NS-2330)-陌孚医药/Medlife

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Tesofensine (Synonyms: NS-2330)

目录号: PL11254 纯度: ≥99%

CAS No. :195875-84-4

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中文名称	Tesofensine
中文别名	(4AR,7AR)-八氢-6-(苯甲基)-1H-吡咯并[3,4-B]吡啶;1-(4-硝基苯基)-1H-吡唑-3-羧酸乙酯;特索芬辛
英文名称	Tesofensine
英文别名	Tesofensine;(1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8- azabicyclo[3.2.1]octane;NS 2330;(1S,3S,4R,5R)-3-(3,4-dichlorophenyl)-4-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane;Tesofensine
Cas No.	195875-84-4
分子式	C₁₇H₂₃NOCl₂
分子量	328.28
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

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; IC 50 =6.5 nM), norepinephrine (NE;IC 50 =1.7 nM), and serotonin (5-HT;IC 50 =11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

性状

Solid

IC50 & Target[1][2]

DA/NE/5-HT

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

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)

ClinicalTrial

参考文献

[1]. Lieuwe Appel, et al. Tesofensine, a novel triple monoamine re-uptake inhibitor with anti-obesity effects: dopamine transporter occupancy as measured by PET. Eur Neuropsychopharmacol. 2014 Feb;24(2):251-61.
[2]. Ann A Coulter, et al. Centrally Acting Agents for Obesity: Past, Present, and Future. Drugs. 2018 Jul;78(11):1113-1132.

溶解度数据	In Vitro: DMSO : 2 mg/mL (6.09 mM; Need ultrasonic and warming)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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