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  2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. MSI-1436

MSI-1436 是具有選擇性的 PTP1B 的非競爭性抑制劑，其 IC50 為 1 μM，而對(duì) TCPTP 的 IC50 值為 224 μM。

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MSI-1436 Chemical Structure

MSI-1436 Chemical Structure

CAS No. : 186139-09-3

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規(guī)格 價(jià)格 是否有貨
500 μg ￥3000
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MSI-1436 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of MSI-1436:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).

IC50 & Target

IC50: 1 μM (PTB1B), 224 μM (TCPTP)[1]
體外研究
(In Vitro)

在 HepG2 中，單獨(dú)的 MSI-1436 (10 μM，30 分鐘) 對(duì) IRβ 的磷酸化沒有影響，但與 100 nM 胰島素聯(lián)合使用時(shí)，MSI-1436 使 p-IRβ 比未處理的細(xì)胞高 18 倍，比處理過的細(xì)胞高約三倍單獨(dú)使用胰島素。MSI-1436 對(duì) TCPTP 的抑制比對(duì) PTP1B 活性的影響低約兩個(gè)對(duì)數(shù)，由此產(chǎn)生的 IC50 值為 224 μM[1]。MSI-1436 (Trodusquemine，10 μM) 在 F11 神經(jīng)元細(xì)胞中恢復(fù) ERK 磷酸化以響應(yīng) mGluR1/5 激動(dòng)劑 DHPG。MSI-1436 (10 uM) 挽救 DHPG 誘導(dǎo)的保持電流并恢復(fù) LMO4KO BLA 神經(jīng)元中的 DSI[2]。MSI-1436 (0.1-100 μM) 阻斷 PTP1B 活性，在培養(yǎng)的神經(jīng)元細(xì)胞中具有胰島素樣作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

MSI-1436 (10 mg/kg，ip) 導(dǎo)致肥胖依賴性體重，降低小鼠的全身脂肪含量和脂肪細(xì)胞大小以及白色脂肪組織的脂質(zhì)含量。MSI-1436 處理可顯著降低血漿胰島素水平。MSI-1436 (10 mg/kg，腹腔注射) 使 STAT-3 的磷酸化增加 2.7 倍，與 100 U/kg 胰島素聯(lián)合使用時(shí)，p-IRβ 比單獨(dú)使用胰島素處理的大鼠增加三倍[1]。MSI-1436 (Trodusquemine) 通過恢復(fù)杏仁核內(nèi)的內(nèi)源性大麻素 (eCB) 信號(hào)而表現(xiàn)出抗焦慮作用[2]。MSI-1436 (5 mg/kg，ip) 對(duì)糖尿病小鼠具有抗糖尿病作用，足以抑制 CD1 小鼠的食物攝入并導(dǎo)致體重減輕[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

685.06

同用名

Trodusquemine; Aminosterol-1436

Formula

C37H72N4O5S
CAS 號(hào)
性狀

固體

顏色

White to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料

純度: ≥95.0%

參考文獻(xiàn)
Animal Administration
[1]

Mice
Male AKR/J mice are randomLy placed on ad libitum 10, 45, or 60% fat kcal diets. After -14 weeks, mice are randomly assigned to three treatment groups (n=5-8 mice/group); MSI-1436 (initial dose of 10 mg/kg with three subsequent weekly doses of 5 mg/kg, intraperitoneally), vehicle (saline, 10 mL/kg, weekly 4×), or pair-fed (PF). PF animals are injected with saline (weekly 4×) and allotted the amount of food consumed daily by MSI-1436-treated animals. On day 23, mice are anesthetized and euthanized for blood and tissue collection, respectively. Plasma is obtained following centrifugation of blood 14,000 rpm for 10 min at 4°C.
Rats
Nine-week-old male Sprague-Dawley rats (225-260 g) with ad libitum access to normal rodent chow are dosed intraperitoneally with MSI-1436 (10 mg/kg, IP) or saline. After an overnight fast, the rats are dosed intraperitoneally with saline or 100 U/kg of insulin. At 30 min after dose, animals are killed, and hypothalami are harvested and homogenized in 1 mL of tissue extraction reagent plus phosphatase and protease inhibitors. Samples are centrifuged (14,000 rpm for 10 min at 4°C), and the protein content of the supernatants are quantitated via BCA kit.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

MSI-1436 相關(guān)分類

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量   濃度   體積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MSI-1436
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HY-12219
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