TMPA---AMPK Activator


Catalog No. size PriceQuantity
M60072-2D 10 mM DMSO (0.526 mL) $119
M60072-2S 2 mg solid $119
M60072-10S 10mg solid $476

Description

TMPA is a novel small molecule that binds to orphan Nuclear Receptor Nur77 with high affinity (Kd = 1.45 ± 0.35 μM), and interferes with the Nur77-LKB1 interaction. TMPA’s binding to Nur77 results in the release and shuttling of LKB1 to the cytoplasm to phosphorylate AMPKα. TMPA treatment can effectively reduce blood glucose and alleviate insulin resistance in type II db/db and high-fat diet– and streptozotocin-induced diabetic mice but not in diabetic littermates with the Nur77 gene knocked out. TMPA may serve as a powerful chemical tool to attain a mechanistic understanding of the regulation of LKB1-AMPK axis and a lead compound for the design and development of therapeutics to treat metabolic diseases.

Product information

CAS Number: 1258275-73-8

Molecular Weight: 380.48

Formula: C21H32O6

Chemical Name: ethyl 2-(2,3,4-trimethoxy-6-octanoylphenyl)acetate

Smiles: CCOC(=O)CC1C(OC)=C(OC)C(=CC=1C(=O)CCCCCCC)OC

InChiKey: WCYMJQXRLIDSAQ-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

TMPA was used at 10 µM final concentration in vitro and in cellular assays.

In Vivo:

TMPA was intraperitoneally (IP) dosed to mice at 50 mg/kg once per day. Formulation: 5.0% (v/v) Tween-80 in 0.9% (w/v) saline.

References:

  1. Zhang YY, et al. The orphan nuclear receptor Nur77 regulates LKB1 localization and activates AMPK. (2012) Nat Chem Biol. 8(11):897-904.

Products are for research use only. Not for human use.


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