MSI-1436 lactate|1309370-86-2|(Trodusquemine lactate; Aminosterol-1436 lactate)-陌孚医药/Medlife

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MSI-1436 lactate (Synonyms: Trodusquemine lactate; Aminosterol-1436 lactate)

目录号: PL09624 纯度: ≥99%

CAS No. :1309370-86-2

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中文名称	MSI-1436 lactate
中文别名	(3Β,5Α,7Α,24R)-3-[[3-[[4-[[3-氨基丙基)氨基]丁基]氨基]丙基]氨基]-胆甾烷-7,24-二醇 24-(硫酸氢酯) 2-羟基丙酸盐;化合物 T12117
英文名称	MSI-1436 lactate
英文别名	MSI-1436 lactate;Aminosterol-1436 lactate;Trodusquemine lactate
Cas No.	1309370-86-2
分子式	C₄₀H₇₈N₄O₈S
分子量	775.13
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

MSI-1436 lactate 是具有选择性的 PTP1B 的非竞争性抑制剂，其 IC₅₀ 值为 1 μM，而对 TCPTP 的 IC₅₀ 值为 224 μM。

生物活性

MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC 50 of 1 μM, 200-fold preference over TCPTP (IC 50 of 224 μM).

性状

Solid

IC50 & Target[1][2]

IC50: 1 μM (PTB1B), 224 μM (TCPTP)

体外研究(In Vitro)

MSI-1436s inhibition of TCPTP is approximately two logs less than the effect on PTP1B activity, with a resulting IC50 value of 224 μM. MSI-1436 (Trodusquemine, 10 μM) restores ERK phosphorylation in response to mGluR1/5 agonist DHPG in F11 neuronal cells. MSI-1436 (10 uM) rescues DHPG-induced holding currents and restores DSI in LMO4KO BLA neurons. MSI-1436 (0.1-100 μM) blocks PTP1B activity. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

MSI-1436 (10 mg/kg, i.p.) causes obesity-dependent body weight, reduces total body fat content and adipocyte size and lipid content of white adipose tissue of mice. MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala. MSI-1436 (5 mg/kg, i.p.) has an anti-diabetic effect on diabetic mice, and is sufficient to suppress food intake and cause weight loss in CD1 mice. 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, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Lantz KA, et al. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-1523.
[2]. Qin Z, et al. Chronic stress induces anxiety via an amygdalar intracellular cascade that impairs endocannabinoid signaling. Neuron. 2015 Mar 18;85(6):1319-31.

溶解度数据	In Vitro: DMSO : 54 mg/mL (53.99 mM; Need ultrasonic and warming)0.1 M HCL : 50 mg/mL (49.99 mM; ultrasonic and adjust pH to 4 with HCl)配制储备液

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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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