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

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

Cat. No.: HY-12219A Purity: ≥95.0%
Handling Instructions

MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).

For research use only. We do not sell to patients.

MSI-1436 lactate Chemical Structure

MSI-1436 lactate Chemical Structure

CAS No. : 1309370-86-2

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1 mg USD 600 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
50 mg USD 6000 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MSI-1436 lactate:

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Publications Citing Use of MCE MSI-1436 lactate

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  • Purity & Documentation

  • References

  • Customer Review

Description

MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), 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]

In Vitro

MSI-1436's inhibition of TCPTP is approximately two logs 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].

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

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[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].

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

Clinical Trial
Molecular Weight

1000.17

Formula

C₃₇H₇₂N₄O₅S . ₇/₂C₃H₆O₃

CAS No.

1309370-86-2

SMILES

NCCCNCCCCNCCCN[[email protected]@H]1C[[email protected]@](C[[email protected]@H](O)[[email protected]]2([H])[[email protected]]3([H])CC[[email protected]@]4(C)[[email protected]@]2([H])CC[[email protected]@]4([[email protected]](C)CC[[email protected]@H](OS(=O)(O)=O)C(C)C)[H])([H])[[email protected]]3(C)CC1.O=C(O)C(C)O.[3.5]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 54 mg/mL (53.99 mM; Need ultrasonic and warming)

H2O : ≥ 33.33 mg/mL (33.32 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[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].

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

Animal Administration
[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].

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

References
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Keywords:

MSI-1436TrodusquemineAminosterol-1436MSI1436MSI 1436Aminosterol1436Aminosterol 1436PhosphataseInhibitorinhibitorinhibit

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Product Name:
MSI-1436 lactate
Cat. No.:
HY-12219A
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