TMPA - ≥98% , CAS No.1258275-73-8

CAS: 1258275-73-8 Cat. No.: T651653 分子式: C₂₁H₃₂O₆ 分子量: 380.48

グレード＆純度 ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

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.

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. ?\nTMPA (10 μM; 6 h) enhances the LKB1-AMPKα interaction but decreases the LKB1-Nur77 interaction under physio logical conditions in Lo2 cells. ?\nTMPA binds directly to LBD in specific conformation. ?\nTMPA (10, 20 μM; 6 h) induces LKB1 nuclear export to activate AMPKα in Lo2 cells. ?\nTMPA (10, 50, 100 μM; 4 h) impairs human T-cell RICD (restimulation-induced cell death). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell Line: Hepatic LO2 cells Concentration: 10, 20 µM Incubation Time: 6 h Result: Led to an increase of LKB1 phosphorylation at Ser428. Western Blot AnalysisCell 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 . 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) . 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.

Form:Solid

仕様

仕様と純度

≥98%

生化学的・生理学的メカニズム

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 stre

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

純度

≥98%

名前と識別子

カノニカル・スマイル

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

分子量

380.48

化学的性質と物理的性質

• 溶解度: DMSO : ≥ 100 mg/mL (262.83 mM)

よくある質問

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1258275-73-8, the molecular formula is C21H32O6, and the molecular weight is 380.48 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.