| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| 体外研究 (In Vitro) |
晚期糖基化终末产物 (AGE) 可导致 β 细胞坏死和 caspase-3 增加。吡格列酮（0.5 或 1 μM，5 天）可以完全防止这些影响，防止 AGE 损害胰腺 β 细胞系 HIT-T15 的活力。吡格列酮（1 μM，1 小时）可以降低 AGE 培养细胞中的 GSSG/GSH 比率，并增加低葡萄糖浓度触发的胰岛素分泌 [2]。
|
|---|---|
| 体内研究 (In Vivo) |
吡格列酮，每天口服一次，持续 14 天，剂量为 10 或 30 mg/kg，可改善糖尿病和胰岛素抵抗；这种作用在肝脏中可能依赖于脂质运载蛋白，但在骨骼肌中则不依赖[3]。吡格列酮（口服灌胃，10 mg/kg，每日一次，持续四周）可以缓解与之相关的血脂异常，提高血糖水平，并显着减轻体重（BW）和心脏肥厚[4]。
|
| 动物实验 |
Animal/Disease Models: ob/ob and adipo-/- ob/ob mice with a C57Bl/6 background[3]
Doses: 10 or 30 mg/kg Route of Administration: po (oral gavage); one time/day; 14 days Experimental Results: demonstrated no changes of serum- free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo-/- ob/ob C57BL/6 mice at 10 mg/kg but Dramatically decreased to a similar degree at 30 mg/kg. Also demonstrated no changes of expressions of TNFα and resistin in adipose tissues of ob/ob and adipo-/- ob/ob mice at 10 mg/kg but diminished at 30 mg/kg. Animal/Disease Models: Male Wistar albino rats[4] Doses: 10 mg/kg Route of Administration: po (oral gavage); one time/day; 4 weeks Experimental Results: diminished the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB), TGF-β1 gene expression and regulated the expression of MMP-2/TIMP-2 system. |
| 参考文献 |
[1]. Kuwabara K, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose leve
[2]. Puddu A, et al. Pioglitazone attenuates the detrimental effects of advanced glycation end-products in the pancreatic beta cell line HIT-T15. Regul Pept. 2012 Aug 20;177(1-3):79-84. [3]. Kubota N, et al. Pioglitazone ameliorates insulin resistance and diabetes by both adiponectin-dependent and -independent pathways. J Biol Chem. 2006 Mar 31;281(13):8748-55. [4]. Elrashidy RA, et al. Pioglitazone attenuates cardiac fibrosis and hypertrophy in a rat model of diabetic nephropathy. J Cardiovasc Pharmacol Ther. 2012 Sep;17(3):324-33. |
| 分子式 |
C19H20N2O3S
|
|
|---|---|---|
| 分子量 |
356.44
|
|
| CAS号 |
111025-46-8
|
|
| 相关CAS号 |
Pioglitazone-d4;1134163-29-3;Pioglitazone hydrochloride;112529-15-4;Pioglitazone potassium;1266523-09-4;Pioglitazone-d4 (alkyl);1134163-31-7
|
|
| SMILES |
O=C(N1)SC(CC2=CC=C(OCCC3=NC=C(CC)C=C3)C=C2)C1=O
|
|
| 别名 |
|
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外) |
|
|||
|---|---|---|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: 2.08 mg/mL (5.84 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (28.06 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), Suspened solution; with ultrasonication. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL | |
| 5 mM | 0.5611 mL | 2.8055 mL | 5.6110 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8055 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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 ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04501406 | Recruiting | Drug: Pioglitazone Other: Placebo |
Type 2 Diabetes Mellitus (T2DM) Nonalcoholic Steatohepatitis |
University of Florida | December 15, 2020 | Phase 2 |
| NCT05775380 | Recruiting | Drug: Pioglitazone 45 mg | Myocardial Reperfusion Injury | University of Campinas, Brazil | June 15, 2023 | Phase 4 |
| NCT03080480 | Terminated | Drug: Pioglitazone | Chronic Granulomatous Disease | Children's Hospital of Fudan University | September 1, 2017 | Phase 1 Phase 2 |
| NCT04535700 | Completed | Drug: Pioglitazone 30 mg Other: standard of care |
Type 2 Diabetes | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal |
September 18, 2020 | Phase 4 |
|
|
|
Clofibric Acid
Rosiglitazone
Alpinetin
Oroxin A
InvivoChem的所有产品仅用于作科学研究，不面向患者销售
Copyright 2020 InvivoChem LLC | All Rights Reserved 粤ICP备20063088号-1
NMR
粤公网安备 44011102003439号