Pioglitazone Hydrochloride

Product Name

Pioglitazone Hydrochloride

CAS No.

112529-15-4

Molecular Weight

392.90

Target

PPARδ

Synonyms

U 72107A; AD 4833

Formula

C19H21ClN2O3S

Appearance

Solid

Purity

99.75%

SMILES

CCC1=CN=C(CCOC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1.Cl

Description

Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

In Vitro Activity

AGEs-induced beta cell necrosis is completely abrogated by adding Pioglitazone to the AGEs culture medium. Furthermore Pioglitazone completely prevented any AGEs-induced increment in caspase-3 activation, thereby restoring caspase-3 activity to the same levels as the control cells. As expected AG is able to counteract AGEs-induced impaired viability.

In Vivo Activity

The serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo-/- ob/ob mice are unchanged after 10 mg/kg Pioglitazone but are significantly reduced to a similar degree after 30 mg/kg Pioglitazone. Moreover, the expressions of TNFα and resistin in adipose tissues of ob/ob and adipo-/- ob/ob mice are unchanged after 10 mg/kg Pioglitazone but are decreased after 30 mg/kg Pioglitazone. Thus, Pioglitazone-induced amelioration of insulin resistance and diabetes may occur adiponectin dependently in the liver and adiponectin independently in skeletal muscle. Pioglitazone (10 mg/kg per d) treatment significantly attenuates the loss of body weight (BW) and cardiac hypertrophy. Pioglitazone treatment significantly reduces the elevated serum glucose levels and markedly improved the associated dyslipidemia. Furthermore, there is a slight but significant increase in serum creatinine level in D rats over their N controls (P <0.05). However, a marked renal dysfunction is observed in diabetic nephropathic (DN) group (P<0.05). Moreover, DN rats exhibits the highest serum activity of CK-MB, relative to both N and D rats (P<0.05). Pioglitazone is able to decrease the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB).

Storage

4 °C, sealed storage, away from moisture In solvent : -80 °C, 6 months; -20 °C, 1 month (sealed storage, away from moisture)

Shipping

Room temperature in continental US; may vary elsewhere.