Pioglitazone D4
(Synonyms: 匹格列酮-D4,U 72107-d4) 目录号 : GC61187An internal standard for the quantification of pioglitazone
Cas No.:1134163-29-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pioglitazone-d4 is intended for use as an internal standard for the quantification of pioglitazone by GC- or LC-MS. Pioglitazone is an agonist of the peroxisome proliferator-activated receptor γ (PPARγ; EC50 = ~500-600 nM for both human and murine PPARγ).1,2 It is selective for PPARγ over PPARα, exhibiting low level activation of PPARα at 1 ?M and 5.4-fold activation at a concentration of 10 ?M.1 Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 μM.3 In vivo, pioglitazone (0.3-3 mg/kg per day) reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats.4 It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model.5 Pioglitazone (2.5 mg/kg) also decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress, indicating antidepressant-like activity that can be reversed by the PPARγ antagonist GW 9662 .6
1.Sakamoto, J., Kimura, H., Moriyama, S., et al.Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazoneBiochem. Biophys. Res. Commun.278(3)704-711(2000) 2.Willson, T.M., Brown, P.J., Sternbach, D.D., et al.The PPARs: From orphan receptors to drug discoveryJ. Med. Chem.43(4)527-550(2000) 3.Shannon, C.E., Daniele, G., Galindo, C., et al.Pioglitazone inhibits mitochondrial pyruvate metabolism and glucose production in hepatocytesFEBS J.284(3)451-465(2017) 4.Sugiyama, Y., Taketomi, S., Shimura, Y., et al.Effects of pioglitazone on glucose and lipid metabolism in Wistar fatty ratsArzneimittelforschung.40(3)263-267(1990) 5.Suzuki, S., Mori, Y., Nagano, A., et al.Pioglitazone, a peroxisome proliferator-activated receptor γ agonist, suppresses rat prostate carcinogenesisInt. J. Mol. Sci.17(12)pii: E2071(2016) 6.Zhao, Q., Wu, X., Yan, S., et al.The antidepressant-like effects of pioglitazone in a chronic mild stress mouse model are associated with PPARγ-mediated alteration of microglial activation phenotypesJ. Neuroinflammation13(1)259(2016)
Cas No. | 1134163-29-3 | SDF | |
别名 | 匹格列酮-D4,U 72107-d4 | ||
Canonical SMILES | O=C(N1)SC(CC2=C([2H])C([2H])=C(OCCC3=NC=C(CC)C=C3)C([2H])=C2[2H])C1=O | ||
分子式 | C19H16D4N2O3S | 分子量 | 360.46 |
溶解度 | DMF: 2.5 mg/ml,DMSO: 2.5 mg/ml | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7742 mL | 13.8712 mL | 27.7423 mL |
5 mM | 0.5548 mL | 2.7742 mL | 5.5485 mL |
10 mM | 0.2774 mL | 1.3871 mL | 2.7742 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Liquid chromatography and tandem mass spectrometry method for quantitative determination of pioglitazone and its metabolite 5-hydroxy pioglitazone in human plasma
Ann Pharm Fr 2017 Mar;75(2):105-111.PMID:27659416DOI:10.1016/j.pharma.2016.07.005.
A liquid chromatography tandem mass spectrometry (LC-MS/MS) based method was developed for the simultaneous estimation of pioglitazone and its active metabolites in human plasma for applicability to pharmacokinetic studies. The chromatographic separation was carried on the reversed phase Peerless Basic C18, column (100×4.6mm, 5μm) at column temperature of 40°C using a binary mobile phase consisting of methanol: 5mM ammonium acetate in 0.1% formic acid (80:20, v/v). The mobile phase was run at a flow rate of 1mL/min and the sample injection was 10μL. The method utilized Pioglitazone D4 (IS1) and 5-hydroxyl pioglitazone M-IV D4 (IS2) as an internal standard. The linearity of the method was validated over the range of 6.04-1503.21ng/mL for pioglitazone and 6.01-1496.28ng/mL for 5-hydroxyl pioglitazone. The mean extraction recovery of PIO & HPIO from the spiked plasma was found to be 94.92% for pioglitazone and 96.13% for 5-hydroxy pioglitazone. The developed method can be successfully employed in healthy human volunteers to monitor the pharmacokinetics profile of pioglitazone.