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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(jìng)爭(zhēng)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
詢問(wèn)價(jià)格 & 貨期

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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(méi)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(guò)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(guò)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

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
目錄號(hào)：
HY-12219
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