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

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

製品番号: HY-12219A 純度: 98.79%
COA 取扱説明書 Technical Support

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

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MSI-1436 lactate

MSI-1436 lactate 構造式

CAS 番号 : 1309370-86-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 2002 在庫あり
Solution
10 mM * 1 mL in DMSO USD 2002 在庫あり
Solid
1 mg $600 在庫あり
5 mg $1140 在庫あり
10 mg $1820 在庫あり
25 mg $3650 在庫あり
50 mg $5850 在庫あり
100 mg $8800 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 8 publication(s) in Google Scholar

Other Forms of MSI-1436 lactate:

MSI-1436 lactate 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

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製品説明

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

IC50 & Target

IC50: 1 μM (PTB1B), 224 μM (TCPTP)[1]
体外実験

MSI-1436's inhibition of TCPTP is less than the effect on PTP1B activity, with a resulting IC50 value of 224 μM[1]. 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[2]. MSI-1436 (0.1-100 μM) blocks PTP1B activity[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MSI-1436 lactate 関連抗体
体内実験

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[1].
MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala[2].
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[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1000.17

分子式

C40H78N4O8S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

NCCCNCCCCNCCCN[C@@H]1C[C@@](C[C@@H](O)[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@]4([C@H](C)CC[C@@H](OS(=O)(O)=O)C(C)C)[H])([H])[C@]3(C)CC1.O=C(O)C(C)O.[3.5]
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 54 mg/mL (53.99 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

0.1 M HCl : 50 mg/mL (49.99 mM; ultrasonic and adjust pH to 4 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9998 mL 4.9992 mL 9.9983 mL
5 mM 0.2000 mL 0.9998 mL 1.9997 mL
10 mM 0.1000 mL 0.4999 mL 0.9998 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 3 mg/mL (3.00 mM); Clear solution

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 98.79%

COA (252 KB) HNMR (194 KB) RP-HPLC (247 KB) MS (71 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[1]

Quantitation of phosphatase activity is measured using an intact cell assay. Hep G2 cells are pretreated with 10 μM MSI-1436 lactate or sodium orthovanadate (100 μM, postive control) for 10 min at 37 °C, then incubated with 10 μM pNPP (a cell permeable hydrolysable substrate) for 30 min at 37 °C. Samples of the supernatants are spectrophotometrically analyzed at OD405 for hydolyzed pNP, a direct end product of phosphatase activity[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[1]

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 to 8 mice/group); MSI-1436 lactate (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 lactate -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[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
0.1 M HCl / DMSO 1 mM 0.9998 mL 4.9992 mL 9.9983 mL 24.9958 mL
5 mM 0.2000 mL 0.9998 mL 1.9997 mL 4.9992 mL
10 mM 0.1000 mL 0.4999 mL 0.9998 mL 2.4996 mL
15 mM 0.0667 mL 0.3333 mL 0.6666 mL 1.6664 mL
20 mM 0.0500 mL 0.2500 mL 0.4999 mL 1.2498 mL
25 mM 0.0400 mL 0.2000 mL 0.3999 mL 0.9998 mL
30 mM 0.0333 mL 0.1666 mL 0.3333 mL 0.8332 mL
40 mM 0.0250 mL 0.1250 mL 0.2500 mL 0.6249 mL
DMSO 50 mM 0.0200 mL 0.1000 mL 0.2000 mL 0.4999 mL
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MSI-1436 lactate Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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.

Keywords:

MSI-14361309370-86-2TrodusquemineAminosterol-1436MSI1436MSI 1436Aminosterol1436Aminosterol 1436PhosphataseInhibitorinhibitorinhibit

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