316371-84-3
316371-84-3 structure
- Name: UNII:2V3E7D3089
- Chemical Name: potassium,5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidin-3-ide-2,4-dione
- CAS Number: 316371-84-3
- Molecular Formula: C18H18KN3O3S
- Molecular Weight: 395.517
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2017-02-12 06:45:01
- Modify Date: 2025-08-21 11:26:33
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Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
| Name | potassium,5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidin-3-ide-2,4-dione |
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| Synonyms |
UNII:2V3E7D3089
Potassium 5-(4-{2-[methyl(2-pyridinyl)amino]ethoxy}benzyl)-4-oxo-4,5-dihydro-1,3-thiazol-2-olate 2,4-Thiazolidinedione, 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-, potassium salt (1:1) |
| Description | Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7]. |
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| Related Catalog | |
| Target |
PPARγ:40 nM (Kd) PPARγ:60 nM (EC50) TRPC5:30 μM (EC50) TRPM3 |
| In Vitro | Rosiglitazone potassium (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes[1]. Rosiglitazone potassium (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons[3]. Rosiglitazone potassium (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[3]. Rosiglitazone potassium (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[4]. Rosiglitazone potassium (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation[7]. Rosiglitazone potassium (5 μM, 7 days) suppresses Olaparib (HY-10162)‑induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells[7]. Cell Proliferation Assay[7] 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[3] Cell Line: Hippocampal neurons Concentration: 1 μM Incubation Time: 24 h Result: Increased NF-α1 and BCL-2 protein level. |
| In Vivo | Rosiglitazone potassium (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats[5]. Rosiglitazone potassium (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[6]. Rosiglitazone potassium (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models[7]. Animal Model: Streptozotocin (STZ)-induced diabetic rats[5] 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[6] 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. |
| References |
| Molecular Formula | C18H18KN3O3S |
|---|---|
| Molecular Weight | 395.517 |
| Exact Mass | 395.070587 |
| PSA | 88.04000 |
| LogP | 2.60550 |
| Hazard Codes | Xi |
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