Pioglitazone

製品コードS2590 バッチS259001

化学情報

	Synonyms	AD-4833, U 72107	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₉H₂₀N₂O₃S
	分子量	356.44	CAS No.	111025-46-8
Solubility (25°C)*	体外	DMSO	15 mg/mL (42.08 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	Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.
in vitro	Pioglitazone is metabolised mainly by CYP2C8 and to a lesser extent by CYP3A4 in vitro. ^[1]
in vivo	Pioglitazone significantly attenuates left ventricular (LV) cavity dilatation and dysfunction by echocardiography as well as LV end-diastolic pressure in mice with extensive anterior myocardial infarction. Pioglitazone partially normalizes LV dP/dt(max) and dP/dt(min), indices of LV contractile function, which are significantly reduced in MI mice. ^[2] Pioglitazone results in a reduced activation of microglia, reduced induction of iNOS-positive cells and less glial fibrillary acidic protein positive cells in both striatum and substantia nigra pars compacta of MPTP mouse model of Parkinson's disease. Pioglitazone almost completely blocks staining of TH-positive neurons for nitrotyrosine, a marker of NO-mediated cell damage. ^[3] Pioglitazone (approximately 20 mg/kg/day) attenuates the MPTP-induced glial activation and prevents the dopaminergic cell loss in the substantia nigra pars compacta (SNpc) in MPTP mouse model of Parkinson's disease. ^[4] Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of 10-month-old APPV717I transgenic mice. Pioglitazone treatment reduces the expression of the proinflammatory enzymes cyclooxygenase 2 (COX2) and inducible nitric oxide synthase (iNOS). Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels, and also a 27% reduction in the levels of soluble Abeta1-42 peptide. ^[5]

製品説明

Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.

in vitro

Pioglitazone is metabolised mainly by CYP2C8 and to a lesser extent by CYP3A4 in vitro. ^[1]

in vivo

Pioglitazone significantly attenuates left ventricular (LV) cavity dilatation and dysfunction by echocardiography as well as LV end-diastolic pressure in mice with extensive anterior myocardial infarction. Pioglitazone partially normalizes LV dP/dt(max) and dP/dt(min), indices of LV contractile function, which are significantly reduced in MI mice. ^[2]

Pioglitazone results in a reduced activation of microglia, reduced induction of iNOS-positive cells and less glial fibrillary acidic protein positive cells in both striatum and substantia nigra pars compacta of MPTP mouse model of Parkinson's disease. Pioglitazone almost completely blocks staining of TH-positive neurons for nitrotyrosine, a marker of NO-mediated cell damage. ^[3]

Pioglitazone (approximately 20 mg/kg/day) attenuates the MPTP-induced glial activation and prevents the dopaminergic cell loss in the substantia nigra pars compacta (SNpc) in MPTP mouse model of Parkinson's disease. ^[4]

Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of 10-month-old APPV717I transgenic mice. Pioglitazone treatment reduces the expression of the proinflammatory enzymes cyclooxygenase 2 (COX2) and inducible nitric oxide synthase (iNOS). Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels, and also a 27% reduction in the levels of soluble Abeta1-42 peptide. ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PASMCs
	濃度	5 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 C57/Bl6 mice
	投薬量	20 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

: , , Mol Nutr Food Res, 2017, doi: 10.1002/mnfr.201601075

: , , Drug Metab Dispos, 2014, 42(3):318-22.

: Data from [Data independently produced by , , J Biol Chem, 2019, 293(43):16572-16582]

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：

Upregulation of PGC-1α expression by pioglitazone mediates prevention of sepsis-induced acute lung injury [ Braz J Med Biol Res, 2024, 57:e13235]	PubMed: 38511769
Mitigation of non-alcoholic steatohepatitis via recombinant Orosomucoid 2, an acute phase protein modulating the Erk1/2-PPARγ-Cd36 pathway [ Cell Rep, 2023, 42(7):112697]	PubMed: 37355990
Molecular Signature Predictive of Long-Term Liver Fibrosis Progression to Inform Antifibrotic Drug Development [ Gastroenterology, 2022, 162(4):1210-1225]	PubMed: 34951993
Artificial intelligence-rationalized balanced PPARα/γ dual agonism resets dysregulated macrophage processes in inflammatory bowel disease [ Commun Biol, 2022, 5(1):231]	PubMed: 35288651
Adipose Rheb deficiency promotes miR-182-5p expression via the cAMP/PPARγ signaling pathway [ J Genet Genomics, 2022, S1673-8527(22)00133-3]	PubMed: 35550871
FGF21 attenuates pulmonary arterial hypertension via downregulation of miR-130, which targets PPARγ [ J Cell Mol Med, 2022, 10.1111/jcmm.17154]	PubMed: 34989130
Peroxisome proliferator-activated receptor-γ ameliorates neuronal ferroptosis after traumatic brain injury in mice by inhibiting cyclooxygenase-2 [ Exp Neurol, 2022, 354:114100]	PubMed: 35490721
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258]	PubMed: 35207746
The downregulation of miR-129-5p relieves the inflammatory response in acute respiratory distress syndrome by regulating PPARγ-mediated autophagy [ Ann Transl Med, 2022, 10(6):345]	PubMed: 35433953
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y]	PubMed: 35118583

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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