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Rosiglitazone

Catalog No. T0334 CAS 122320-73-4

Synonyms: BRL49653

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

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Rosiglitazone, CAS 122320-73-4

Pack Size	Availability	Price/USD
25 mg	In stock	$ 33.00
50 mg	In stock	$ 47.00
100 mg	In stock	$ 82.00
200 mg	In stock	$ 147.00
500 mg	In stock	$ 246.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.87%

Purity: 99.43%

Purity: 99.35%

Purity: 98.61%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.
Targets&IC50	PPARγ2:100 nM(EC50), PPARγ:60 nM(EC50), PPARγ1:30 nM(EC50)
In vitro	Rosiglitazone reduces bone formation rate and increases adipose content within the bone marrow. It decreases the expression of osteoblast-specific genes Runx2/Cbfa1, DLX5, and α1(I) collagen, while expression of the adipocyte-specific fatty acid binding protein AP2 is increased. This drug leads to significant bone loss, evidenced by reductions in bone mass, trabecular width, and number, along with an increase in trabecular separation. Furthermore, in ob/ob mice, rosiglitazone enhances transcription of genes encoding mitochondrial proteins in white adipocytes, which is accompanied by changes in mitochondrial number and structure.
In vivo	In certain cell lines, Rosiglitazone reduces cholesterol synthesis independent of peroxisome proliferator-activated receptor γ (PPARγ). The compound significantly enhances the phosphorylation of threonine 172 in the α subunit of AMP-dependent protein kinase, increasing the AMP: ATP ratio. Additionally, Rosiglitazone boosts secretion of adiponectin by up to 2.3-fold from omental cells, while secretion from subcutaneous fat cells remains unaffected. In 3T3-L1 adipocytes, Rosiglitazone alters mitochondrial morphological characteristics and protein profile. It activates complexes containing α1- and α2-AMPK, leading to a marked increase in phosphorylation of acetyl-CoA carboxylase. Rosiglitazone also acts as a dominant inhibitor of osteoblastogenesis from mouse marrow in vitro through the activation of PPAR-gamma2.
Cell Research	Rosiglitazone is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Human neuroblastoma SH-SY5Y cells are maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100 μg/mL Streptomycin and 100 U/mL Penicillin G. SH-SY5Y cells are transfected with the longest isoform of human tau (2N4R) tagged with GFP using lipofectamine. 24 hr after transfection, cells are treated with Rosiglitazone (10 μM, 50 μM) for 24 hr[2].

Synonyms	BRL49653
Molecular Weight	357.43
Formula	C18H19N3O3S
CAS No.	122320-73-4

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. HCl: 35.7 mg/mL (100 mM)

DMSO: 35.7 mg/mL (100 mM)

References and Literature

1. Cellai I, et al. Antineoplastic effects of rosiglitazone and PPARgamma transactivation in neuroblastoma cells. Br J Cancer. 2006 Oct 9;95(7):879-88. 2. Lin CF, et al. Rosiglitazone regulates anti-inflammation and growth inhibition via PTEN. Biomed Res Int. 2014;2014:787924. 3. García-Ruiz I, et al. Effects of rosiglitazone on the liver histology and mitochondrial function in ob/ob mice. Hepatology. 2007 Aug;46(2):414-23. 4. Wiggin TD, et al. Rosiglitazone treatment reduces diabetic neuropathy in streptozotocin-treated DBA/2J mice. Endocrinology. 2008 Oct;149(10):4928-37. 6. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. 7. Qiu Y, Sun Y, Xu D, et al. Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue[J]. EBioMedicine. 2018, 37: 344-355. 8. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks[J]. Chemical Science. 2020, 11(7): 1775-1797.

Citations

1. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks. Chemical Science. 2020, 11(7): 1775-1797. 2. Miao Y, Wu X, Xue X, et al. Morin, the PPARγ agonist, inhibits Th17 differentiation by limiting fatty acid synthesis in collagen-induced arthritis. Cell Biology and Toxicology. 2022: 1-20. 3. Qiu Y, Sun Y, Xu D, et al. Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue. EBioMedicine. 2018, 37: 344-355. 4. Miao Y, Geng Y, Yang L, et al. Morin inhibits the transformation of fibroblasts towards myofibroblasts through regulating “PPAR-γ-glutaminolysis-DEPTOR” pathway in pulmonary fibrosis. The Journal of Nutritional Biochemistry. 2021: 108923. 5. Miao Y, Zhang C, Yang L, et al. The activation of PPARγ enhances Treg responses through up-regulating CD36/CPT1-mediated fatty acid oxidation and subsequent N-glycan branching of TβRII/IL-2Rα. Cell Communication and Signaling. 2022, 20(1): 1-22 6. Li J, Bai Y, Liu Y, et al.Transcriptome-based chemical screens identify CDK8 as a common barrier in multiple cell reprogramming systems.Cell Reports.2023, 42(6). 7. Chen S, Zhou X, Li W, et al.Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression.Biochemical Pharmacology.2023: 115800. 8. Schöckel L, Woischke C, Surendran S A, et al.PPARG activation promotes the proliferation of colorectal cancer cell lines and enhances the antiproliferative effect of 5-fluorouracil.BMC cancer.2024, 24(1): 1-12. 9. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Traditional Chinese Medicine Monomer Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Approved Drug Library Orally Active Compound Library

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Keywords

Rosiglitazone 122320-73-4 Apoptosis Autophagy DNA Damage/DNA Repair Membrane transporter/Ion channel Metabolism Ferroptosis PPAR TRP/TRPV Channel diabetic neuroprotection senescence PPARγ Inhibitor cancer diabetes BRL-49653 HCC antihyperglycemic TRP Channel bladder mellitus Peroxisome proliferator-activated receptors inhibit BRL49653 BRL 49653 carcinoma smoke ovarian cancer Transient receptor potential channels hepatocellular inhibitor

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