[CAS NO. 1258275-73-8] TMPA
PRODUCTS SPECIFICATIONS [1258275-73-8]
DESCRIPTION [1258275-73-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 380.48 |
| Molecular Formula | C21H32O6 |
| SMILES | COC1=C(CC(OCC)=O)C(C(CCCCCCC)=O)=CC(OC)=C1OC |
1 Publications Citing Use of MCE
Summary
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] .
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male C57BL/KsJ-Lepr db /Lepr db (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. |
Appearance
Solid
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
DMSO : ≥ 100 mg/mL ( 262.83 mM )
* "≥" means soluble, but saturation unknown.
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 |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution
References