Rosiglitazone Hydrochloride

Product Name

Rosiglitazone Hydrochloride

CAS No.

302543-62-0

Molecular Weight

393.89

Synonyms

BRL 49653 hydrochloride

Formula

C18H20ClN3O3S

SMILES

[H]Cl.O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O

Description

Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer.

In Vitro Activity

Rosiglitazone hydrochloride (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes. Rosiglitazone hydrochloride (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone hydrochloride (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner. Rosiglitazone hydrochloride (0.01-100 μM, 15 min) inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively. Rosiglitazone hydrochloride (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation. Rosiglitazone hydrochloride (5 μM, 7 days) suppresses Olaparib‑induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells. Cell Proliferation Assay Cell Line: A2780 and SKOV3 cells Concentration: 0.5-50 μM Incubation Time: 1-7 days Result: Inhibited cell proliferation in a time‑dependent and concentration‑dependent manner. Western Blot Analysis Cell Line: Hippocampal neurons Concentration: 1 μM Incubation Time: 1 μM Result: Increased NF-α1 and BCL-2 protein level.

In Vivo Activity

Rosiglitazone hydrochloride (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats. Rosiglitazone hydrochloride (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats. Rosiglitazone hydrochloride (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere.