Rosiglitazone

製品コードS2556 バッチS255602

化学情報

	Synonyms	BRL 49653	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₁₉N₃O₃S
	分子量	357.43	CAS No.	122320-73-4
Solubility (25°C)*	体外	DMSO	72 mg/mL (201.43 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
in vitro	Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. Rosiglitazone has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. Rosiglitazone activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase. ^[1] Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.^[2] Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. ^[3] Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes. ^[4]
in vivo	Rosiglitazone administration results in significant bone loss, including a decrease in bone volume, trabecular width, and trabecular number and an increase in trabecular spacing. Rosiglitazone also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. Rosiglitazone decreases the expression of the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen, whereas the expression of the adipocyte-specific fatty acid binding protein aP2 is increased. ^[2] Rosiglitazone upregulates gene transcripts encoding mitochondrial proteins in white adipocytes from ob/ob mice accompanied by an increase in mitochondrial mass and changes in mitochondrial structure. ^[4]

製品説明

Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.

in vitro

Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. Rosiglitazone has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. Rosiglitazone activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase. ^[1]

Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.^[2]

Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. ^[3]

Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes. ^[4]

in vivo

Rosiglitazone administration results in significant bone loss, including a decrease in bone volume, trabecular width, and trabecular number and an increase in trabecular spacing. Rosiglitazone also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. Rosiglitazone decreases the expression of the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen, whereas the expression of the adipocyte-specific fatty acid binding protein aP2 is increased. ^[2]

Rosiglitazone upregulates gene transcripts encoding mitochondrial proteins in white adipocytes from ob/ob mice accompanied by an increase in mitochondrial mass and changes in mitochondrial structure. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Primary neutrophils
	濃度	10 μM
	反応時間
	実験の流れ	Cells were treated with indicated concentration of drug.
動物実験	動物モデル	Male Sprague dawely rats
	投薬量	5 mg/kg
	投与方法	p.o.

参考

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カスタマーフィードバック

: Data from [J Leukoc Biol, 2014, 95(4), 587-98]

: Data from [J Leukoc Biol, 2014, 95(4), 587-98]

: Data from [Data independently produced by , , Theranostics, 2018, 8(15):4262-4278]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429]	PubMed: 38365899
Celastrol Stabilizes Glycolipid Metabolism in Hepatic Steatosis by Binding and Regulating the Peroxisome Proliferator-Activated Receptor γ Signaling Pathway [ Metabolites, 2024, 14(1)64]	PubMed: 38276299
LCN2 secreted by tissue-infiltrating neutrophils induces the ferroptosis and wasting of adipose and muscle tissues in lung cancer cachexia [ J Hematol Oncol, 2023, 16(1):30]	PubMed: 36973755
Blockade of IL-6R prevents preterm birth and adverse neonatal outcomes [ EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865]	PubMed: 37944273
KLF2/PPARγ axis contributes to trauma-induced heterotopic ossification by regulating mitochondrial dysfunction [ Cell Prolif, 2023, e13521.]	PubMed: 37340819
Transcriptomic Analysis Reveals Fibroblast Growth Factor 11 (FGF11) Role in Brown Adipocytes in Thermogenic Regulation of Goats [ Int J Mol Sci, 2023, 24(13)10838]	PubMed: 37446019
Transcriptomic Analysis Reveals Fibroblast Growth Factor 11 (FGF11) Role in Brown Adipocytes in Thermogenic Regulation of Goats [ Int J Mol Sci, 2023, 24(13)10838]	PubMed: 37446019
IL-23 signaling prevents ferroptosis-driven renal immunopathology during candidiasis [ Nat Commun, 2022, 13(1):5545]	PubMed: 36138043
Snail acetylation by autophagy-derived acetyl-coenzyme A promotes invasion and metastasis of KRAS-LKB1 co-mutated lung cancer cells [ Cancer Commun (Lond), 2022, 42(8):716-749]	PubMed: 35838183
Snail acetylation by autophagy-derived acetyl-coenzyme A promotes invasion and metastasis of KRAS-LKB1 co-mutated lung cancer cells [ Cancer Commun (Lond), 2022, 10.1002/cac2.12332]	PubMed: 35838183

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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