| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Rosiglitazone (HSDB-7555; BRL-49653; TDZ-01; TDZ01; trade name Avandia) is an approved antidiabetic drug of the thiazolidinedione class with antidiabetic properties and potential antineoplastic activity. It is also a potent insulin sensitizer with IC50s of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. It is also a selective PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively.
| ln Vitro |
Pluripotent C3H10T1/2 stem cells are differentiated into adipocytes by rosiglitazone (0.1–10 μM, 72 h) [1]. When combined with the NF-α1 promoter, rosiglitazone (1 μM, 24 h) stimulates PPARγ, which in turn activates gene transcription in neurons [3]. Hippocampal neurons and Neuro2A cells are shielded from oxidative stress by rosiglitazone (1 μM, 24 hours), which also increases BCL-2 expression in an NF-κ1-dependent way [3]. With IC50 values of 9.5 and 4.6 μM, rosiglitazone (0.01-100 μM, 15 minutes) inhibits TRPM3, hence preventing PregS- and nifedipine-induced activity, respectively [4]. The proliferation of ovarian cancer cells is inhibited by rosiglitazone (0.5-50 μM, 7 days) [7]. In A2780 and SKOV3 cells, rosiglitazone (5 μM, 7 days) suppresses Olaparib-induced cellular senescence alterations and stimulates apoptosis [7].
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| ln Vivo |
In diabetic rats, oral rosiglitazone (5 mg/kg, once day for 8 weeks) lowers blood glucose levels [5]. By activating PPARγ and RXRα, rosiglitazone (ip, 3 mg/kg/day) lowers blood glucose and inhibits airway inflammation brought on by M1 macrophage polarization in male Wistar rats [6]. In A2780 and SKOV3 animal subcutaneous xenograft models, rosiglitazone (ip, 10 mg/kg, every 2 days) suppresses the growth of subcutaneous ovarian cancer [7].
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| Cell Assay |
Cell Proliferation Assay[7]
Cell Types: A2780 and SKOV3 cells Tested Concentrations: 0.5-50 μM Incubation Duration: 1-7 days Experimental Results: Inhibited cell proliferation in a time‑dependent and concentration‑dependent manner. Western Blot Analysis[3] Cell Types: Hippocampal neurons Tested Concentrations: 1 μM Incubation Duration: 24 h Experimental Results: Increased NF-α1 and BCL-2 protein level. |
| Animal Protocol |
Animal/Disease Models: Streptozotocin (STZ)-induced diabetic rats[5]
Doses: 5 mg/kg Route of Administration: Oral administration, daily for 8 weeks. Experimental Results: diminished 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/Disease Models: Male Wistar rats[6] Doses: 3 mg/kg/day Route of Administration: intraperitoneal (ip)injection, twice a day, 6 days Consecutive per week for 12 weeks Experimental Results: 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 diminished the ratio of M1/M2. |
| 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.
[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. [3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [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. [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. [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. [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. |
| Molecular Formula |
C18H19N3O3S
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| Molecular Weight |
357.43
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| CAS # |
122320-73-4
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| Related CAS # |
Rosiglitazone maleate;155141-29-0;Rosiglitazone hydrochloride;302543-62-0;Rosiglitazone potassium;316371-84-3;Rosiglitazone-d3;1132641-22-5
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| SMILES |
O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O
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| InChi Key |
YASAKCUCGLMORW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)
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| Chemical Name |
5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)benzyl)thiazolidine-2,4-dione
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| Synonyms |
HSDB7555; TDZ 01; HSDB 7555; HSDB-7555; BRL 49653; BRL49653; BRL-49653; TDZ-01; TDZ01; Rosiglitazone. trade name Avandia.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7978 mL | 13.9888 mL | 27.9775 mL | |
| 5 mM | 0.5596 mL | 2.7978 mL | 5.5955 mL | |
| 10 mM | 0.2798 mL | 1.3989 mL | 2.7978 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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