| Field | Specification |
|---|---|
| Target | |
| Alternative names | BRL 49653 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H19N3O3S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Rosiglitazone, also known as BRL 49653, is an orally active, selective PPARγ agonist (EC50 60 nM, Kd 40 nM) with blood-brain barrier permeability. It also activates TRPC5 (EC50 30 μM) and inhibits TRPM3. It can be used in research on obesity and diabetes, senescence, and ovarian cancer[1][2][4][7][8]. It is supplied as a white to off-white solid (C18H19N3O3S, MW 357.43) at 99.94% purity.
Physical & Chemical Properties
| CAS Number | 122320-73-4 |
|---|---|
| Molecular Formula | C18H19N3O3S |
| Molecular Weight | 357.43 g/mol |
| Purity | 99.94% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O |
| Target | PPARγ, TRPC5, TRPM3 |
| Signaling Pathway | Cell Cycle/DNA Damage; Vitamin D Related/Nuclear Receptor; Metabolic Enzyme/Protease; Membrane Transporter/Ion Channel; Neuronal Signaling; Autophagy; Apoptosis |
| Solubility | In Vitro: DMSO: 175 mg/mL (489.61 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Ethanol: 2 mg/mL (5.60 mM; Requires sonication and warming and heat to 60°C) H2O: < 0.1 mg/mL (insoluble) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
[1][2][4]
|
PPARγ 40 nM (Kd) |
PPARγ 60 nM (EC50) |
TRPC5 30 μM (EC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 175 mg/mL (489.61 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| Ethanol | 2 mg/mL (5.60 mM) | requires sonication and warming and heat to 60°C |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 5 mg/mL (13.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 5 mg/mL (13.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (13.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Protocol 4
| Composition | 5% DMSO + 40% PEG300 + 5% Tween-80 + 50% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (6.99 mM); clear solution |
Protocol 5
| Composition | 5% DMSO + 95% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (6.99 mM); clear solution |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 6
| Composition | 0.5% CMC-Na/saline water |
|---|---|
| Result | 10 mg/mL (27.98 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
In pluripotent C3H10T1/2 stem cells, Rosiglitazone (0.1-10 μM, 72 h) drives differentiation into adipocytes[1]. Rosiglitazone (1 μM, 24 h) activates PPARγ, and PPARγ then binds the NF-α1 promoter, driving gene transcription in neurons[3]. In Neuro2A cells and hippocampal neurons, Rosiglitazone (1 μM, 24 h) protects against oxidative stress and raises BCL-2 expression in a manner dependent on NF-α1[3]. Rosiglitazone (0.01-100 μM, 15 min) blocks TRPM3; the IC50 values are 9.5 and 4.6 μM against nifedipine-evoked and PregS-evoked activity, respectively[4]. Rosiglitazone (0.5-50 μM, 7 days) reduces the proliferation of ovarian cancer cells[7]. In A2780 and SKOV3 cells, Rosiglitazone (5 μM, 7 days) suppresses the Olaparib induced changes in cellular senescence and promotes apoptosis[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 (oral administration, 5 mg/kg, daily for 8 weeks) lowers serum glucose in diabetic rats[5]. In male Wistar rats, Rosiglitazone (intraperitoneal injection, 3 mg/kg/day) ameliorates cigarette smoke-induced airway inflammation by inhibiting M1 macrophage polarization through activation of PPARγ and RXRα[6]. In A2780 and SKOV3 mouse subcutaneous xenograft models, Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) suppresses growth of subcutaneous ovarian cancer[7]. After experimental traumatic brain injury, Rosiglitazone can exert neuroactive effects when given by intraperitoneal injection, and can modulate astrocyte polarization and neuroinflammation in a PPAR-γ dependent manner[8].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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