Rosiglitazone (BRL 49653)

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は、ラット、3T3-L1、ヒト脂肪細胞に対してそれぞれ12、4、9 nMのIC50を持つ強力な血糖降下薬であり、強力なチアゾリジンジオン系インスリン感受性向上薬です。RosiglitazoneはPPAR-gammaの純粋なリガンドであり、PPAR-alpha結合作用はありません。RosiglitazoneはTRP channelsを調節し、autophagyを誘導します。Rosiglitazoneはferroptosisを予防します。
in vitro	Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. This compound has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. It activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase. This chemical activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro. It increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. This compound changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes.
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. This compound also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. It 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. This chemical 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.

製品説明

Rosiglitazoneは、ラット、3T3-L1、ヒト脂肪細胞に対してそれぞれ12、4、9 nMのIC50を持つ強力な血糖降下薬であり、強力なチアゾリジンジオン系インスリン感受性向上薬です。RosiglitazoneはPPAR-gammaの純粋なリガンドであり、PPAR-alpha結合作用はありません。RosiglitazoneはTRP channelsを調節し、autophagyを誘導します。Rosiglitazoneはferroptosisを予防します。

in vitro

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

This chemical activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.

It increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected.

This compound changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes.

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. This compound also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. It 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.

This chemical 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.

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 this compound.
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

https://pubmed.ncbi.nlm.nih.gov/11994296/
https://pubmed.ncbi.nlm.nih.gov/14500573/
https://pubmed.ncbi.nlm.nih.gov/12466369/

https://pubmed.ncbi.nlm.nih.gov/15520860/
https://pubmed.ncbi.nlm.nih.gov/21406603/
https://pubmed.ncbi.nlm.nih.gov/30737476/
https://pubmed.ncbi.nlm.nih.gov/35131600/
https://pubmed.ncbi.nlm.nih.gov/28892640/

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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：

Adipocytes orchestrate obesity-related chronic inflammation through β2-microglobulin [ Signal Transduct Target Ther, 2025, 10(1):394]	PubMed: 41330906
Vesicle-associated membrane protein 5 is an intrinsic defense factor for embryonic stem cells against coronaviruses [ Nat Commun, 2025, 16(1):6241]	PubMed: 40624080
Compromised Peroxisome Proliferator-Activated Receptor γ-Mediated Impaired Placental Glucose Transport Via the Phosphatidylinositol 3-Kinase/Protein Kinase B Signaling Pathway Is Associated With Fetal Growth Restriction [ Lab Invest, 2025, 105(4):104103]	PubMed: 39909142
Rosiglitazone-Mediated Activation of PPARγ Induces PlGF Expression in Trophoblast Cells [ Reprod Sci, 2025, 32(6):1864-1875]	PubMed: 40295383
Comparative Study of Porcine Mesenchymal Stem Cells Behavior and Lipid Metabolism on Plant-Based Scaffolds and Two-Dimensional Systems for Cultivated Fat [ Eng Life Sci, 2025, 25(10):e70050]	PubMed: 41098339
Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429]	PubMed: 38365899
Adipocyte inflammation is the primary driver of hepatic insulin resistance in a human iPSC-based microphysiological system [ Nat Commun, 2024, 15(1):7991]	PubMed: 39266553
Brain Short-Chain Fatty Acids Induce ACSS2 to Ameliorate Depressive-Like Behavior via PPARγ-TPH2 Axis [ Research (Wash D C), 2024, 7:0400]	PubMed: 38939042
Inhibition of Selenoprotein I promotes ferroptosis and reverses resistance to platinum chemotherapy by impairing Akt phosphorylation in ovarian cancer [ MedComm (2020), 2024, 5(12):e70033]	PubMed: 39669976
TCP1 expression alters the ferroptosis sensitivity of diffuse large B-cell lymphoma subtypes by stabilising ACSL4 and influences patient prognosis [ Cell Death Dis, 2024, 15(8):611]	PubMed: 39174525

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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