yingweiwo

TMPA

Alias: TMPA
Cat No.:V33400 Purity: ≥98%
TMPA is a high-affinity Nur77 antagonist, and binding to Nur77 results in the release and shuttling of LKB1 in the cytoplasm to activate AMPKα.
TMPA
TMPA Chemical Structure CAS No.: 1258275-73-8
Product category: AMPK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Product Description
TMPA is a high-affinity Nur77 antagonist, and binding to Nur77 results in the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA can effectively lower blood glucose and alleviate insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA can reduce RICD of human T cells and can also be utilized in the research on cancer and T cell apoptosis disorders.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
TMPA (5, 10, 20, 40, 80 μM; 6 hours or 10 μM; 0.5, 1, 3, 6, 12, 24, 36, 48 hours) antagonizes Nur77-LKB1 ligated TMPA ( 10 μM; 6 hours) improves the LKB1-AMPKα response but lowers the LKB1-Nur77 response in Lo2 cells under physiological conditions [1]. TMPA directly interacts with LBD with a specific structural picture [1]. TMPA (10, 20 μM; 6 h) promotes LKB1 nuclear export and activates AMPKα in Lo2 cells [1]. TMPA (10, 50, 100 μM; 4 h) damages human T cells RICD (restimulation-induced [1].
ln Vivo
In individuals with type II diabetes, TMPA (50 mg/kg; intraperitoneal injection; single dose daily for 19 days) can lower blood pressure and enhance diabetic tolerance [1].
Cell Assay
Cell viability assay [2]
Cell Types: T cell
Tested Concentrations: 10, 50, 100 μM
Incubation Duration: 4 h
Experimental Results: Dramatically diminished T cell RICD (cell death) in a dose-dependent manner [2].

Western Blot Analysis[1]
Cell Types: Liver LO2 Cells
Tested Concentrations: 10, 20 µM
Incubation Duration: 6 hrs (hours)
Experimental Results:
Experimental Results: Increased LKB1 Ser428 phosphorylation.

Western Blot Analysis[1]
Cell Types: Liver LO2 cells
Tested Concentrations: 5, 10, 20, 40, 80 µM
Incubation Duration: 6 hrs (hours)
Experimental Results: AmPKα phosphorylation increased in a dose- and time-dependent manner. At a concentration of 10 µM, the LKB1-AmPKα interaction is rescued by reducing the nur77-lKb1 interaction.
Animal Protocol
Animal/Disease Models: Male C57BL/KsJ-Leprdb/Leprdb (db/db ) mice (10 weeks old; type II diabetes model) [1].
Doses: 50 mg/kg
Route of Administration: intraperitoneal (ip) injection; daily for 19 days.
Experimental Results: Blood glucose diminished Dramatically on day 7 and persisted for the remainder of the test. Increases the amount of phosphorylated AMPKα in mouse liver.
References

[1]. The orphan nuclear receptor Nur77 regulates LKB1 localization and activates AMPK. Nat Chem Biol. 2012 Nov;8(11):897-904.

[2]. Modulation of T-cell apoptosis by small molecule compounds targeting the nuclear orphan receptor Nur 77. (2018).

Additional Infomation
Ethyl (2,3,4-trimethoxy-6-octanoylphenyl)acetate is an aromatic ketone.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H32O6
Molecular Weight
380.4752
Exact Mass
380.219
CAS #
1258275-73-8
Related CAS #
1258275-73-8
PubChem CID
60146245
Appearance
Light yellow to yellow solid
Density
1.1±0.1 g/cm3
Boiling Point
480.0±45.0 °C at 760 mmHg
Flash Point
205.8±28.8 °C
Vapour Pressure
0.0±1.2 mmHg at 25°C
Index of Refraction
1.491
LogP
5.25
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
14
Heavy Atom Count
27
Complexity
438
Defined Atom Stereocenter Count
0
SMILES
O=C(C1=C([H])C(=C(C(=C1C([H])([H])C(=O)OC([H])([H])C([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H]
InChi Key
WCYMJQXRLIDSAQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H32O6/c1-6-8-9-10-11-12-17(22)15-13-18(24-3)21(26-5)20(25-4)16(15)14-19(23)27-7-2/h13H,6-12,14H2,1-5H3
Chemical Name
ethyl 2-(2,3,4-trimethoxy-6-octanoylphenyl)acetate
Synonyms
TMPA
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ≥ 100 mg/mL (262.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.2628 mL 1.3141 mL 2.6283 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Contact Us