Rosiglitazone HCl

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rosiglitazone (BRL 49653) hydrochloride 是一种具有口服活性的 PPARγ 选择性激动剂 (EC50: 60 nM, Kd: 40 nM)。Rosiglitazone hydrochloride 是一种 TRPC5 激活剂 (EC50: 30 μM) 和 TRPM3 抑制剂。Rosiglitazone hydrochloride 可用于肥胖、糖尿病、衰老、卵巢癌的研究。

Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

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 (HY-10162)?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 AnalysisCell Line:Hippocampal neurons Concentration:1 μM Incubation Time:1 μM Result:Increased NF-α1 and BCL-2 protein level.

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. 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).

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Immunology/Inflammation

IκB kinase (IKK)

PPAR

Metabolic Disease

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302543-62-0

393.89

C18H19N3O3S·HCl

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (158.67 mM)

Cl.CN(CCOC1=CC=C(CC2SC(=O)NC2=O)C=C1)C1=CC=CC=N1

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(-20℃)

With Ice Pack

≥ 2 years