Pioglitazone

別名：AD-4833, U 72107

製品コード：S2590 純度：99.83%

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.

CAS No. 111025-46-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
200mg	JPY 85500	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（33）

製品安全説明書

現在のバッチを見る：純度： 99.83%

99.83

Pioglitazone関連製品

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シグナル伝達経路

PPARシグナル伝達経路

PPAR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HEK293T	Function assay	1 uM	24 hrs	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay	21030263
HEK293	Function assay	10 uM	24 hrs	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	24890090
THP1	Function assay	10 uM	24 hrs	Upregulation of ABCA1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control	27220065
THP1	Function assay	10 uM	24 hrs	Upregulation of ABCG1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control	27220065
PC3	Function assay	50 uM	24 hrs	Increase in p21(WAF1) protein expression in human PC3 cells at 50 uM incubated for 24 hrs by Western blot analysis	28395220
MDA-MB-231	Function assay	50 uM	24 hrs	Increase in p21(WAF1) protein expression in human MDA-MB-231 cells at 50 uM incubated for 24 hrs by Western blot analysis	28395220
SCC15	Cytotoxicity assay	50 uM	24 hrs	Cytotoxicity against human SCC15 cells transfected with PPARalpha siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	29031063
SCC15	Cytotoxicity assay	50 uM	24 hrs	Cytotoxicity against human SCC15 cells transfected with PPARbeta siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	29031063
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in AP1 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in CD36 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in Glut4 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
K562-IMA[r]	Function assay	10 uM	72 hrs	Induction of sensitization to imatinib-induced cytotoxicity in imatinib-resistant human K562-IMA[r] cells assessed as induction of cell death at 10 uM after 72 hrs in presence of 1 uM imatinib by propidium iodide/Triton-X100 dye based FACS analysis	31648125
3T3L1	Function assay	100 umol/L		Increase in PPARgamma mRNA levels in mouse 3T3L1 cells at 100 umol/L by RT-PCR	20392645
HepG2	Function assay	30 uM		Binding affinity to NAF1 (unknown origin) expressed in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	30770154
HepG2	Function assay	30 uM		Binding affinity to NAF1 in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	30770154
Cos7	Function assay		14 hrs	Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay, EC50=0.3μM	20307981
CHO	Function assay		24 hrs	Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay, EC50=0.39μM	21377875
HepG2	Function assay		20 hrs	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay, EC50=0.57μM	22341573
HEK293	Function assay		18 hrs	Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay, EC50=0.8μM	23102891
THP1	Antiinflammatory assay		1 hr	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA, IC50=18.84μM	23811092
THP1	Antiinflammatory assay		2 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA, IC50=18.6μM	24531227
HEK293	Function assay		18 hrs	Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay, EC50=0.21μM	25333853
COS7	Function assay		42 hrs	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.5μM	27560282
COS7	Function assay		42 hrs	Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay, EC50=0.32μM	27569195
COS7	Function assay		42 hrs	Transactivation of Gal4 fused human PPARgamma LBD expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.38μM	27918994
HEK293	Function assay		24 hrs	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=1.1μM	28465099
HEK293	Function assay		4 hrs	Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay, IC50=22μM	28465099
HepG2	Function assay		24 hrs	Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay, EC50=0.24μM	30001846
HEK293BENA	Function assay		24 hrs	Transactivation of GAL4-fused human PPARgamma transfected in HEK293BENA cells after 24 hrs by steady glo-luciferase reporter gene assay, EC50=2.053μM	30351933
HEK293	Function assay		18 hrs	Transactivation of human full length PPARgamma expressed in HEK293 cells after 18 hrs by luciferase reporter gene based luminescence assay, EC50=0.1μM	30362739
293H	Function assay		16 hrs	Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay, EC50=0.098μM	30429097
stem cells	Function assay		5 days	Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production measured on day 5 in presence of IDX by ELISA, EC50=0.35μM	30672698
HEK293T	Function assay		18 hrs	Transactivation of full length human PPARgamma2 expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.25μM	30676741
HEK293T	Function assay		18 hrs	Transactivation of chimeric Gal4 yeast DBD fused-PPARgamma LBD (unknown origin) expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.35μM	30676741
COS7	Function assay		39 hrs	Transactivation of Gal4-fused human PPARgamma transfected in COS7 cells co-transfected with pGAL5-TK-pGL3 and pRennilla-CMV incubated for 39 hrs by dual luciferase reporter assay, EC50=1.4μM	31648125
CV-1	Function assay			In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.69μM	8576907
3T3-L1	Function assay			Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.16μM	9599241
CV-1	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.58884μM	9836620
CV-1	Function assay			Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay., EC50=0.58μM	11720854
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay	16680159
CV1	Function assay			Transactivation of PPARgamma in CV1 cells, EC50=0.55μM	16821769
CHO	Function assay			Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay, EC50=0.14μM	20656494
COS-1	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.39μM	21130649
COS7	Function assay			Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50=0.3μM	21873070
Sf21	Function assay			Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50=0.3μM	21965623
Sf21	Function assay			Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50=2μM	21965623
COS7	Function assay			Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay, EC50=0.2μM	23130964
COS7	Function assay			Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay, EC50=0.2μM	26595749
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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.

Targets

PPARγ ^[2]

In Vitro
In vitro	Pioglitazone is metabolised mainly by CYP2C8 and to a lesser extent by CYP3A4 in vitro. ^[1]
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	p-VEGFR2 / VEGFR Phopsho-RB / RB		29972411

In Vivo
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]
動物実験	動物モデル	Male C57/Bl6 mice
	投与量	20 mg/kg
	投与経路	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05946564	Not yet recruiting	ANCA Associated Vasculitis\|Rapidly Progressive Glomerulonephritis\|Crescentic Glomerulonephritis	Assistance Publique - Hôpitaux de Paris\|Ministry of Health France	July 2023	Phase 3
NCT05305287	Recruiting	Non-Alcoholic Fatty Liver Disease\|Type 2 Diabetes\|Mitochondrial Metabolism Disorders	The University of Texas Health Science Center at San Antonio\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	November 1 2022	Phase 4
NCT05411965	Completed	Diabetes Mellitus Type 2	Boryung Pharmaceutical Co. Ltd	April 28 2022	Phase 1
NCT04501406	Recruiting	Type 2 Diabetes Mellitus (T2DM)\|Nonalcoholic Steatohepatitis	University of Florida\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	December 15 2020	Phase 2
NCT04535700	Completed	Type 2 Diabetes	Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal	September 18 2020	Phase 4
NCT00904046	Recruiting	Uric Acid Kidney Stone Disease	University of Texas Southwestern Medical Center\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|Takeda Pharmaceuticals North America Inc.	September 5 2019	Not Applicable

参考
[1] Jaakkola T, et al. Basic Clin Pharmacol Toxicol,?006, 99(1), 44-51. [2] Shiomi T, et al. Circulation,?002, 106(24), 3126-3132. [3] Dehmer T, et al. J Neurochem,?004, 88(2), 494-501. [4] Breidert T, et al. J Neurochem,?002, 82(3), 615-624. [5] Heneka MT, et al. Brain,?005, 128(Pt 6), 1442-1453. [6] Wang M, et al. J Cell Mol Med. 2022 Feb;26(4):1034-1049. + 展開

参考

+ 展開

化学情報

分子量	356.44	化学式	C₁₉H₂₀N₂O₃S
CAS No.	111025-46-8	SDF	Download Pioglitazone SDFをダウンロードする
Smiles	CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 20 mg/mL ( (56.11 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
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