Rosiglitazone

SKU: orb1226757

Description

A potent and selective PPARγ agonist that binds to the PPARγ ligand-binding domain with a Kd of 40 nM; an antidiabetic agent that has been used as an oral hypoglycemic agent in the treatment of Type II diabetes; also inhibits TRP channels TRPM2 and TRPM3 with IC50 of 22.5 uM and 5-10 uM, respectively; also increases klotho and decreases Wnt5A in tumor cells.Diabetes Approved(In Vitro):Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes.Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons.Rosiglitazone (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 (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 (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation.Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162) induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells.(In Vivo):Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats.Rosiglitazone (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 (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models.

Key Properties

• CAS Number: 122320-73-4
• MW: 357.4268
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉N₃O₃S
• SMILES: O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O
• Target: PPAR
• Solubility: DMSO: ≥ 180 mg/mL

Bioactivity

• In Vivo:
  Animal model: Streptozotocin (STZ)-induced diabetic rats. Dosage: 5 mg/kg. Administration: Oral administration, daily for 8 weeks. Result: Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group. Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups. Animal model: Male Wistar rats. Dosage: 3 mg/kg/day. Administration: Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks. Result: Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS). Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRL-49653

Quick Database Links

Gene Symbol

PPAR