ALEXIS Biochemicals: Pioglitazone

ALX-270-367

Revised 25-Jul-07

Pioglitazone
SYNONYMS	5-[[4-[2-(5-Ethyl-2-pyridinyl)ethoxy]phenyl]methyl-2,4-thiazolidinedione
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PPAR Agonists

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-367-M001		1 mg	48.00 USD
ALX-270-367-M005		5 mg	190.00 USD

Product Specification

FORMULA:	C₁₉H₂₀N₂O₃S
MW:	356.4
CAS NUMBER:	111025-46-8
MERCK INDEX:	14: 7452
PURITY:	≥98% (¹H-NMR)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (2.5mg/ml) or dimethyl formamide (2.5mg/ml).
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C

Product Description

Pioglitazone selectively activates PPARγ-1. It is about one tenth as potent as rosiglitazone (EC₅₀~500nM for human and mouse PPARγ). In a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα, pioglitazone and rosiglitazone exhibit low level activation of PPARα at 1µM and 5.4- and 4.2-fold activation, respectively, at a concentration of 10µM.

Not sold in the US.

Product Specific Literature References

[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents: B.C. Cantello, et al.; J. Med. Chem. 37, 3977 (1994) Abstract
An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma): J.M. Lehmann, et al.; J. Biol. Chem. 270, 12953 (1995) Abstract; Full Text
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones: T.M. Willson, et al.; J. Med. Chem. 39, 665 (1996) Abstract
Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone: J. Sakamoto, et al.; BBRC 278, 704 (2000) Abstract
The PPARs: from orphan receptors to drug discovery: T.M. Willson, et al.; J. Med. Chem. 43, 527 (2000) Abstract

General Information

Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (Prod. No. ALX-350-103) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands.

Further Categories Containing This Product:

Antidiabetic Agents / Related Products

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