中文名称: | 吡格列酮盐酸盐 促销 | ||||
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英文名称: | Pioglitazone hydrochloride | ||||
别名: | 安可妥 5-(4-(2-(5-Ethylpyridin-2-yl)ethoxy)benzyl)thiazolidine-2,4-dione hydrochloride | ||||
CAS No: | 112529-15-4 | 分子式: | C19H20N2O3S.HCl | 分子量: | 392.9 |
CAS No: | 112529-15-4 | ||||
分子式: | C19H20N2O3S.HCl | ||||
分子量: | 392.9 | ||||
MDL: | MFCD04975446 |
基本信息
产品编号: |
P10035 |
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产品名称: |
Pioglitazone hydrochloride |
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CAS: |
112529-15-4 |
储存条件 |
粉末 |
室温 |
四年 |
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分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量 |
392.90 |
-20℃ |
一个月 |
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化学名: |
5-(4-(2-(5-Ethylpyridin-2-yl)ethoxy)benzyl)thiazolidine-2,4-dione hydrochloride |
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Solubility (25°C): |
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体外:
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DMSO |
78mg/mL (198.52mM) |
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Ethanol |
4mg/mL (10.18mM) |
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Water |
Insoluble |
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体内(现配现用): |
1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5mg/mL (6.36mM); Clear solution |
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此⽅案可获得 ≥ 2.5mg/mL (6.36mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 |
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2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5mg/mL (6.36mM); Clear solution |
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此⽅案可获得 ≥ 2.5mg/mL (6.36mM,饱和度未知) 的澄清溶液。以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。 |
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3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.5mg/mL (6.36mM); Clear solution |
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此⽅案可获得 ≥ 2.5mg/mL (6.36mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.5452mL |
12.7259mL |
25.4518mL |
5mM |
0.5090mL |
2.5452mL |
5.0904mL |
10mM |
0.2545mL |
1.2726mL |
2.5452mL |
50mM |
0.0509mL |
0.2545mL |
0.5090mL |
生物活性
产品描述 |
Pioglitazone 是⼀种有效,选择性的 PPARγ 激动剂,⾼亲和⼒结合到 PPARγ 配体结合域。作⽤于⼈和⿏ PPARγ,EC50 分 别为 0.93 和 0.99μM。 |
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靶点 |
Ferroptosis |
hPPARγ 0.93μM(EC50) |
rPPARγ 0.99μM(EC50) |
CYP2C8 1.7μM(Ki) |
CYP3A4 11.8μM(Ki) |
体外研究 |
Pioglitazone抑制LPS诱导的iNOS表达和NO的产生,并抑制iNOS表达足以保护多巴胺神经元抗LPS损伤。Pioglitazone保护多巴胺能神经元免受LPS,至少通过抑制iNOS的表达和NO的产生,这是通过抑制p38蛋白激酶的活性介导的。Pioglitazone抑制p38蛋白的LPS诱导的磷酸化。 |
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体内研究 |
在雄性肥胖鼠中,Pioglitazone口服(0.3-3毫克/公斤/天7天)剂量依赖性地降低了高血糖症,高脂血症,和高胰岛素血症。在大鼠中,Pioglitazone改善葡萄糖耐受性和增加外源性胰岛素和血浆甘油三酯的清除。在未处理的SOD1-G93A小鼠中,Pioglitazone处理转基因小鼠显示改进的肌肉力量和体重,表现出延迟疾病发作和显著较长生存比。在大鼠和小鼠中,Pioglitazone显著降低高血糖症,高脂血症,高胰岛素血症,葡萄糖不耐症,其特征如胰岛素抵抗状态。在黄色的KK小鼠的隔膜和脂肪组织中,Pioglitazone在的胰岛素介导的葡萄糖代谢。在Zucker肥胖大鼠中,Pioglitazone增强在源性胰岛素的血糖反应。在APPV717I转基因小鼠的海马和皮层活性星形细胞中,Pioglitazone导致激活的小胶质细胞的数量减少。在APPV717I转基因小鼠中,Pioglitazone降低β-分泌-1(BACE1)的mRNA和蛋白水平。 |
推荐实验方法(仅供参考)
Cell Assay |
In order to evaluate cell proliferation, HIT-T15 cells are seeded on 96-well plates (3×104 cells/well) and cultured for 5 days as described. Viable cells are determined using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay. To evaluate cell apoptosis and cell necrosis, HIT-T15 cells are plated on 6-well dishes (7×105 cells/well) for 5 days in standard conditions (CTR) or in the presence of AGEs (AGEs) with or without Pioglitazone (0.5 or 1μM) or AG (1mM). They are then processed to measure both the activity of caspase-3 and the activity of lactate dehydrogenase (LDH) (a stable cytosolic enzyme that is a marker of cell membrane damage and cell death due to necrosis) using Cytotox 96 Non Radioactive Cytotoxicity Assay |
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Animal Administration |
Mice 10mg/kg Pioglitazone HCl or vehicle (0.25% carboxymethylcellulose) is adnimistered to ob/ob and adipo-/- ob/ob mice by oral gavage once daily for 14 consecutive days. 30mg/kg Pioglitazone or vehicle is also adnimistered to ob/ob and adipo-/-ob/ob mice by oral gavage once daily for 14 consecutive days. Rats Male Wistar albino rats (weighing 250±20 g) are ued.Rats that achieved serum glucose level ≥250mg/dL and serum creatinine level ≥1.5mg/dL are divided into 2 groups (n=10 per each group): diabetic nephropathic (DN) group in which rats received an equal amount of vehicle (0.5% carboxy methyl cellulose) and Pioglitazone-treated (DN+Pio) group in which rats treated with Pioglitazone. Pioglitazone (10mg/kg BW) is given orally by gastric gavage, once daily, for 4 weeks. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )