| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Rosiglitazone HCl (HSDB-7555; BRL-49653; TDZ-01; BRL49653), the hydrochloride salt of Rosiglitazone, is a potent antidiabetic/antihyperglycemic drug of the thiazolidinedione class with anti-inflammatory activities. It acts as 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 which activates PPARγ1/γ2/γ with EC50s of 30 nM, 100 nM and 60 nM, respectively. Rosiglitazone binds to the PPAR receptors in fat cells and making the cells more responsive to insulin.
| ln Vitro |
Adipocyte differentiation is the outcome of pluripotent C3H10T1/2 stem cells treated with rosiglitazone hydrochloride (0.1–10 μM) for 72 hours[1]. In addition to protecting Neuro2A cells and hippocampal neurons against oxidative stress, Rosiglitazone hydrochloride (1 μM, 24 h) activates PPARγ, which binds to the NF-κ1 promoter to activate gene transcription[3]. It also up-regulates BCL-2 expression. The proliferation of ovarian cancer cells is inhibited by rosiglitazone hydrochloride (0.01-100 Rosiglitazone hydrochloride (0.5-50 μM, 7 days)[7]. In A2780 and SKOV3 cells, 5 μM administered over a 7-day period inhibits changes in cellular senescence caused by Olaparib and encourages apoptosis[7].
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| ln Vivo |
In diabetic rats, rosiglitazone hydrochloride (oral treatment, 5 mg/kg, daily for 8 weeks) lowers serum glucose levels[5]. By suppressing M1 macrophage polarization and activating PPARγ and RXRα in male Wistar rats, rosiglitazone hydrochloride (intraperitoneal injection, 3 mg/kg/day) reduces airway inflammation caused by cigarette smoke[6]. Subcutaneous ovarian cancer growth is inhibited in A2780 and SKOV3 mouse subcutaneous xenograft models by rosiglitazone hydrochloride (intraperitoneal injection, 10 mg/kg, once every two days)[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: 1 μM 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 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.HCL
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| Molecular Weight |
393.89
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| CAS # |
302543-62-0
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| Related CAS # |
Rosiglitazone maleate;155141-29-0;Rosiglitazone;122320-73-4;Rosiglitazone potassium;316371-84-3;Rosiglitazone-d3;1132641-22-5
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| SMILES |
CN(C1=CC=CC=N1)CCOC2=CC=C(CC3C(NC(S3)=O)=O)C=C2.Cl
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| Chemical Name |
5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)benzyl)thiazolidine-2,4-dione hydrochloride
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| Synonyms |
Rosiglitazone HCl; Rosiglitazone Hydrochloride; HSDB-7555; BRL-49653 HCl; BRL49653; TDZ-01; BRL 49653; HSDB 7555; HSDB7555; 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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5388 mL | 12.6939 mL | 25.3878 mL | |
| 5 mM | 0.5078 mL | 2.5388 mL | 5.0776 mL | |
| 10 mM | 0.2539 mL | 1.2694 mL | 2.5388 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00484419 | Completed Has Results | Drug: Colesevelam HCl Drug: rosiglitazone maleate |
Type 2 Diabetes Hyperlipidemia |
Daiichi Sankyo | May 2007 | Phase 3 |
| NCT00672919 | Completed | Drug: Pioglitazone | Diabetes Mellitus | Takeda | November 2003 | Phase 4 |
| NCT00499707 | Completed | Drug: rosiglitazone maleate/metformin hydrochloride |
Diabetes Mellitus, Type 2 | GlaxoSmithKline | October 8, 2003 | Phase 3 |
| NCT00297063 | Completed | Drug: Rosiglitazone | Diabetes Mellitus, Type 2 | GlaxoSmithKline | January 11, 2006 | Phase 3 |
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