Pioglitazone HCl

製品コードS2046 バッチS204604

印刷

化学情報

Chemical Structure Synonyms AD-4833, U-72107E Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H20N2O3S.HCl
分子量 392.9 CAS No. 112529-15-4
Solubility (25°C)* 体外 DMSO 79 mg/mL (201.06 mM)
Ethanol 7 mg/mL (17.81 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
in vitro

Pioglitazone inhibits LPS-induced iNOS expression and NO generation, and inhibition of iNOS is sufficient to protect dopaminergic neurons against LPS insult. Pioglitazone protects dopaminergic neurons against LPS insult at least via inhibiting iNOS expression and NO generation, which is potentially mediated via inhibition of p38 MAPK activity. Pioglitazone inhibits LPS-induced phosphorylation of p38 MAPK. [1]
in vivo

Pioglitazone administered orally (0.3-3 mg/kg/d for 7 days) dose dependently reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in male fatty rats. Pioglitazone improves glucose tolerance and augmentes the glycemic response to exogenous insulin and clearance of plasma triglyceride in rats. [2] Pioglitazone-treated transgenic mice reveals improved muscle strength and body weight, exhibits a delayed disease onset, and survives significantly longer than nontreated SOD1-G93A mice. [3] Pioglitazone markedly decreases hyperglycemia, hyperlipidemia, hyperinsulinemia, and glucoseintolerance characterized as insulin resistant states in these rats and mice. Pioglitazone potentiates insulin-mediated glucose metabolism in the diaphragm and adipose tissues of yellow KK mice and enhanced the glycemic response to exogenous insulin in Zucker fatty rats. [4] Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of APPV717I transgenic mice. Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels in APPV717I transgenic mice. [5]

プロトコル(参考用のみ)

カスタマーフィードバック

, , Mol Nutr Food Res, 2017, 61(9)

Data from [Data independently produced by , , Endocrinology and Metabolism, 2016, 311(4): E763-E771.]

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：

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
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
Rubicon promotes the M2 polarization of Kupffer cells via LC3-associated phagocytosis-mediated clearance to improve liver transplantation [ Cell Immunol, 2022, 378:104556] PubMed: 35700602
Exosomes derived from pioglitazone-pretreated MSCs accelerate diabetic wound healing through enhancing angiogenesis [ J Nanobiotechnology, 2021, 19(1):150] PubMed: 34020670
The Function of PPARγ/AMPK/SIRT-1 Pathway in Inflammatory Response of Human Articular Chondrocytes Stimulated by Advanced Glycation End Products. [ Biol Pharm Bull, 2019, 42(8):1303-1309] PubMed: 31366866
Activation of PPARγ pathway enhances cellular anti-oxidant capacity to protect long-term cultured primary rat neural cells from apoptosis [ Nan Fang Yi Ke Da Xue Xue Bao, 2019, 39(1):23-29] PubMed: 30692062
N-3 polyunsaturated fatty acids increase hepatic fibroblast growth factor 21 sensitivity via a PPAR-γ-β-klotho pathway. [Yang W, et al. Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075] PubMed: 28371258
The Role of Bile Salt Export Pump (BSEP) Gene Repression in Drug-Induced Cholestatic Liver Toxicity [Brandy Garzel, et al. Drug Metab Dispos, 2013, 42(3):318-22] PubMed: 24335466

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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