2. Vitamin D Related/Nuclear Receptor Epigenetics PI3K/Akt/mTOR
  3. Nuclear Hormone Receptor 4A/NR4A AMPK
  4. TMPA

TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation.

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TMPA Chemical Structure

TMPA Chemical Structure

CAS No. : 1258275-73-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 237 In-stock
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10 mM * 1 mL in DMSO USD 237 In-stock
Solid
2 mg USD 132 In-stock
5 mg USD 215 In-stock
10 mg USD 350 In-stock
50 mg USD 850 In-stock
100 mg USD 1300 In-stock
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Based on 1 publication(s) in Google Scholar

TMPA Related Antibodies

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Description

TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation[1][2].

IC50 & Target

Nur77/NR4A1

 

In Vitro

TMPA (5, 10, 20, 40, 80 μM; 6 h or 10 μM; 0.5, 1, 3, 6, 12, 24, 36, 48 h) antagonizes the Nur77-LKB1 interaction in a dose- and time-dependent manner in hepatic LO2 cells[1].
TMPA (10 μM; 6 h) enhances the LKB1-AMPKα interaction but decreases the LKB1-Nur77 interaction under physio logical conditions in Lo2 cells[1].
TMPA binds directly to LBD in specific conformation[1].
TMPA (10, 20 μM; 6 h) induces LKB1 nuclear export to activate AMPKα in Lo2 cells[1].
TMPA (10, 50, 100 μM; 4 h) impairs human T-cell RICD (restimulation-induced cell death)[2].

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

TMPA Related Antibodies

Cell Viability Assay[2]

Cell Line: T cells
Concentration: 10, 50, 100 µM
Incubation Time: 4 h
Result: Significantly reduced T-cell RICD in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Hepatic LO2 cells
Concentration: 10, 20 µM
Incubation Time: 6 h
Result: Led to an increase of LKB1 phosphorylation at Ser428.

Western Blot Analysis[1]

Cell Line: Hepatic LO2 cells
Concentration: 5, 10, 20, 40, 80 µM
Incubation Time: 6 h
Result: Increased the amount of phosphorylation of AmPKα in a dose- and time-dependent manner.
Rescued the LKB1-AmPKα interaction by reducing the nur77-lKb1 interaction when at 10 µM.
In Vivo

TMPA (50 mg/kg; i.p.; single daily for 19 days) is capable of lowering blood glucose and improving glucose tolerance in type II diabetic mice[1].

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

Animal Model: Male C57BL/KsJ-Leprdb/Leprdb (db/db) mice (10-week-old; type II diabetic model)[1].
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; single daily for 19 days.
Result: Significantly reduced blood glucose at day 7 and persisted during the remainder of the test.
Increased the amount of phosphorylated AMPKα in the liver of mice.
Molecular Weight

380.48

Formula

C21H32O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=C(CC(OCC)=O)C(C(CCCCCCC)=O)=CC(OC)=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (262.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6283 mL 13.1413 mL 26.2826 mL
5 mM 0.5257 mL 2.6283 mL 5.2565 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. 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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.
Purity & Documentation
References

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. 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
DMSO 1 mM 2.6283 mL 13.1413 mL 26.2826 mL 65.7065 mL
5 mM 0.5257 mL 2.6283 mL 5.2565 mL 13.1413 mL
10 mM 0.2628 mL 1.3141 mL 2.6283 mL 6.5706 mL
15 mM 0.1752 mL 0.8761 mL 1.7522 mL 4.3804 mL
20 mM 0.1314 mL 0.6571 mL 1.3141 mL 3.2853 mL
25 mM 0.1051 mL 0.5257 mL 1.0513 mL 2.6283 mL
30 mM 0.0876 mL 0.4380 mL 0.8761 mL 2.1902 mL
40 mM 0.0657 mL 0.3285 mL 0.6571 mL 1.6427 mL
50 mM 0.0526 mL 0.2628 mL 0.5257 mL 1.3141 mL
60 mM 0.0438 mL 0.2190 mL 0.4380 mL 1.0951 mL
80 mM 0.0329 mL 0.1643 mL 0.3285 mL 0.8213 mL
100 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6571 mL
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TMPA Related Classifications

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:

TMPA1258275-73-8Nuclear Hormone Receptor 4A/NR4AAMPKNerve Growth Factor IB-like ReceptorAMP-activated protein kinasetype II diabeteshepatic LO2AMPKαLKB1T cellsInhibitorinhibitorinhibit

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