| Identification | Back Directory | [Name]
ROSIGLITAZONEPOTASSIUMSALT | [CAS]
316371-84-3 | [Synonyms]
Rosiglitazone (potassium)
ROSIGLITAZONEPOTASSIUMSALT
LHRPXZBKWPFSIR-UHFFFAOYSA-N
potassium 5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)benzyl)-2,4-dioxothiazolidin-3-ide | [Molecular Formula]
C18H18KN3O3S | [MDL Number]
MFCD28143771 | [MOL File]
316371-84-3.mol | [Molecular Weight]
395.522 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol:2.0(Max Conc. mg/mL);5.06(Max Conc. mM)
H2O:1.0(Max Conc. mg/mL);2.53(Max Conc. mM) | [form ]
A crystalline solid |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| 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.
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| [IC 50]
PPARγ: 40 nM (Kd); PPARγ: 60 nM (EC50); TRPC5: 30 μM (EC50); TRPM3 | [storage]
Store at -20°C | [References]
[1] Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6. DOI:10.1074/jbc.270.22.12953
[2] Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8. DOI:10.1021/jm950395a
[3] Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. DOI:10.1111/jnc.13152
[4] Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30. DOI:10.1124/mol.110.069922
[5] Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. DOI:10.1139/cjpp-2017-0332
[6] Haoshen Feng, et al. Rosiglitazone ameliorated airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα. Int Immunopharmacol. 2021 Aug;97:107809. DOI:10.1016/j.intimp.2021.107809
[7] Zehua Wang, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib. Cancer Chemother Pharmacol. 2020 Feb;85(2):273-284. DOI:10.1007/s00280-019-04025-8 |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
| Company Name: |
Abcam Limited
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| Tel: |
021-2070050 400921018 |
| Website: |
www.abcam.cn |
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