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Submit ReviewRosiglitazone
说明： Potent and selective PPARγ agonist; antidiabetic agent
别名： BRL 49653
化学名： 5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione
纯度： ≥98% (HPLC)
生物活性 for Rosiglitazone
Rosiglitazone is a potent and selective PPARγ agonist (EC50 = 60 nM); exhibits no activity at PPARα and PPARβ. Promotes differentiation of pluripotent C3H10T1/2 stem cells into adipocytes. Also promotes differentiation of urothelial organoids in combination with Erlotinib (Cat. No. 7194). Exhibits antihyperglycemic activity in diabetic ob/ob mouse model. Antidiabetic agent.
化合物库 for Rosiglitazone
Rosiglitazone is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen FDA-Approved Drugs and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Rosiglitazone
| 分子量 | 357.43 |
| 公式 | C18H19N3O3S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 122320-73-4 |
| PubChem ID | 77999 |
| InChI Key | YASAKCUCGLMORW-UHFFFAOYSA-N |
| Smiles | CN(CCOC1=CC=C(CC2SC(NC2=O)=O)C=C1)C3=CC=CC=N3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Rosiglitazone
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.74 | 100 |
制备储备液 for Rosiglitazone
以下数据基于产品分子量 357.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.8 mL | 13.99 mL | 27.98 mL |
| 5 mM | 0.56 mL | 2.8 mL | 5.6 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.8 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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产品说明书 for Rosiglitazone
参考文献 for Rosiglitazone
参考文献是支持产品生物活性的出版物。
Lehmann et al (1995) An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J.Biol.Chem. 270 12953 PMID: 7768881
Willson et al (1996) The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J.Med.Chem. 39 665 PMID: 8576907
Santos et al (2019) Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity. Nat.Commun. 10 4407 PMID: 31562298
If you know of a relevant reference for Rosiglitazone, please let us know.
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关键词: Rosiglitazone, Rosiglitazone supplier, BRL49653, High, affinity, selective, PPAR, agonist, thiazolidinedione, TZD, derivative, antidiabetic, agent, organoids, differentiation, BRL, 49653, PPARgamma, Receptors, Other, Differentiation, Products, Organoids, 5325, Tocris Bioscience
15 篇 Rosiglitazone 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Rosiglitazone 的部分引用包括：
Fellous et al (2020) Phytocannabinoids promote viability and functional adipogenesis of bone marrow-derived mesenchymal stem cells through different molecular targets Biochemical Pharmacology 175 PMID: 32061773
Vitale et al (2018) Fishing for Targets of Alien Metabolites: A Novel Peroxisome Proliferator-Activated Receptor (PPAR) Agonist from a Marine Pest. Mar Drugs 16 PMID: 30400299
Brust et al (2018) A structural mechanism for directing corepressor-selective inverse agonism of PPARγ. Nat Commun 9 4687 PMID: 30409975
Smith et al (2019) Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties. Psychopharmacology (Berl) PMID: 31119329
Vincenzo et al (2021) Beneficial Effects of Akkermansia muciniphila Are Not Associated with Major Changes in the Circulating Endocannabinoidome but Linked to Higher Mono-Palmitoyl-Glycerol Levels as New PPARα Agonists. Cells 10 PMID: 33477821
Vincenzo et al (2021) Three of a Kind: Control of the Expression of Liver-Expressed Antimicrobial Peptide 2 (LEAP2) by the Endocannabinoidome and the Gut Microbiome. Molecules 27 PMID: 35011234
Chang et al (2021) Ketogenic diet prevents paclitaxel-induced neuropathic nociception through activation of PPARγ signalling pathway and inhibition of neuroinflammation in rat dorsal root ganglion. Eur J Neurosci 54 5341-5356 PMID: 34318540
Mark et al (2017) High Concentrations of Rosiglitazone Reduce mRNA and Protein Levels of LRP1 in HepG2 Cells. Front Pharmacol 8 772 PMID: 29201005
Yun-Hee et al (2009) Inhibition of thymic adipogenesis by caloric restriction is coupled with reduction in age-related thymic involution. J Immunol 183 3040-52 PMID: 19648267
Matsa et al (2016) Transcriptome Profiling of Patient-Specific Human iPSC-Cardiomyocytes Predicts Individual Drug Safety and Efficacy Responses In Vitro. Cell Stem Cell. 19 311 PMID: 27545504
Warrick et al (2016) FOXA1, GATA3 and PPARγ Cooperate to Drive Luminal Subtype in Bladder Cancer: A Molecular Analysis of Established Human Cell Lines. Sci Rep 6 38531 PMID: 27924948
Luciano et al (2020) Identification and Characterization of Cannabimovone, a Cannabinoid from Cannabis sativa, as a Novel PPARγ Agonist via a Combined Computational and Functional Study. Molecules 25 PMID: 32138197
Liang et al (2020) Generation of Functional Brown Adipocytes from Human Pluripotent Stem Cells via Progression through a Paraxial Mesoderm State. Cell Stem Cell 27 784-797.e11 PMID: 32783886
Ahlem et al (2011) Studies of the pharmacology of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol, a synthetic anti-inflammatory androstene. Int J Clin Exp Med 4 119 PMID: 21686136
Elisabetta et al (2023) Targeting gut dysbiosis against inflammation and impaired autophagy in Duchenne muscular dystrophy. EMBO Mol Med 15 e16225 PMID: 36594243
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Agonist dose-response analyses of the Human PPAR gamma Assay..
By
GAJANAN KATKAR on 12/07/2019
分析类型： In Vitro
种属： Human
细胞系/组织： PPARg reporter cells
PPAR gamma Assay was performed using manual dispensing and following the protocol described in this Technical Manual, using the Rosiglitazone. PPAR gamma reporter cells treated with 2,500 nM Rosiglitazone yielded an average RLU value with CV=7%, S/B = 162 and a corresponding Z’= 0.78.