Pioglitazone
|
Catalog No.GC14948
One-Click Copy Product Info
|
Pioglitazone은 오르랄 항당뇨제로 사용되는 글리타존 또는 티아조리디논 클래스에 속한다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 111025-46-8
Sample solution is provided at 25 µL, 10mM.
Pioglitazone은 오르랄 항당뇨제로 사용되는 글리타존 또는 티아조리디논 클래스에 속한다. Pioglitazone은 peroxisome proliferator-activated 수용체 γ (PPARγ)의 작용하는 PPARγ의 리간드로 인간과 쥐 PPARγ의 EC50가 각각 0.93과 0.99 µM이다[1-2].
Pioglitazone (10 µM; 4시간)은 고혈당으로 인한 INS-1 세포에서 AMPK 활동의 감소를 되돌렸다[3].Pioglitazone (50 µM; 48시간)은 또한 다세포 종양 구체 배양 시스템 (MCTS)에서의 종양 세포 증식도 억제했다[4].
Pioglitazone (구내 복용, 매일 10이나 30mg/kg 일일 한 번, 14일간)은 인슐린 저항성과 당뇨병을 개선한다[5]. 4주간의 Pioglitazone 치료 (매일 10이나 20mg/kg, 20주에서 24주령부터)는 고지식 식사 (HFD)로 유발된 글루코스대사기능장애, 복측 해마 교질 섬유 산성 단백질 (GFAP)의 상향조절, 복측 해마 CA1 GFAP 면역반응성 뇌섬세포의 총 과정 길이 및 분기점 수의 감소 그리고 쥐의 우울 현상 유형을 완화시킨다[6]. Pioglitazone (구내 복용; 10mg/kg; 매일 한 번, 4주간)은 체중 (BW), 심근비대 혈당 수준을 현저하게 낮추고 관련 지질 비정상 상태를 개선한다[7].
References:
[1]. Kuwabara K, Murakami 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 levels and modifies lipoprotein profiles in KK-Ay mice. J Pharmacol Exp Ther. 2004 Jun;309(3):970-7. doi: 10.1124/jpet.103.064659. Epub 2004 Feb 24. PMID: 14982965.
[2]. Legchenko E, Chouvarine P, et,al. PPARγ agonist pioglitazone reverses pulmonary hypertension and prevents right heart failure via fatty acid oxidation. Sci Transl Med. 2018 Apr 25;10(438):eaao0303. doi: 10.1126/scitranslmed.aao0303. PMID: 29695452.
[3]. Karunakaran U, Elumalai S, et,al. Pioglitazone-induced AMPK-Glutaminase-1 prevents high glucose-induced pancreatic β-cell dysfunction by glutathione antioxidant system. Redox Biol. 2021 Sep;45:102029. doi: 10.1016/j.redox.2021.102029. Epub 2021 Jun 3. PMID: 34107382; PMCID: PMC8187239.
[4]. Gottfried E, Rogenhofer S, et,al. Pioglitazone modulates tumor cell metabolism and proliferation in multicellular tumor spheroids. Cancer Chemother Pharmacol. 2011 Jan;67(1):117-26. doi: 10.1007/s00280-010-1294-0. Epub 2010 Mar 9. PMID: 20217088.
[5]. Kubota N, Terauchi Y, 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. doi: 10.1074/jbc.M505649200. Epub 2006 Jan 23. PMID: 16431926.
[6]. Lam YY, Tsai SF, et,al. Pioglitazone rescues high-fat diet-induced depression-like phenotypes and hippocampal astrocytic deficits in mice. Biomed Pharmacother. 2021 Aug;140:111734. doi: 10.1016/j.biopha.2021.111734. Epub 2021 May 19. PMID: 34022606.
[7]. Elrashidy RA, Asker ME, 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. doi: 10.1177/1074248411431581. Epub 2012 Jan 18. PMID: 22261714.
| 세포 실험 [1]: | |
세포 라인 | INS-1세포 |
제조 방법 | 세포는 Pioglitazone (10 µM)로 처리되었고 고혈당 (30 mM)이 있든 없든 관계없이 처리되었습니다. |
반응 조건 | 10 µM;4시간 동안 |
응용 분야 | Pioglitazone은 고혈당으로 인한 INS-1 세포에서 AMPK 활동의 감소를 역전시켰습니다. |
| 동물 실험 [2]: | |
동물 모형 | C57Bl/6 유전 배경을 가진 ob/ob 및 adipo-/- ob/ob 쥐 |
제조 방법 | 매일 한 번, 14일 연속으로 구내 복용으로 10-30 mg/kg Pioglitazone 또는 운반제 (0.25% carboxymethylcellulose)를 쥐에게 투여했습니다. |
제형 | 10-30 mg/kg; oral gavage; 14 일 동안 |
응용 분야 | 10 mg/kg의 Pioglitazone은 ob/ob 쥐의 인슐린 저항성과 당뇨병을 현저하게 개선할 수 있고 30 mg/kg의 Pioglitazone 투여는 더 좋은 효과를 가집니다. |
참고문헌: [1]. Karunakaran U, Elumalai S, et,al. Pioglitazone-induced AMPK-Glutaminase-1 prevents high glucose-induced pancreatic β-cell dysfunction by glutathione antioxidant system. Redox Biol. 2021 Sep;45:102029. doi: 10.1016/j.redox.2021.102029. Epub 2021 Jun 3. PMID: 34107382; PMCID: PMC8187239.[2]. Kubota N, Terauchi Y, 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. doi: 10.1074/jbc.M505649200. Epub 2006 Jan 23. PMID: 16431926. | |
| Cas No. | 111025-46-8 | SDF | |
| Synonyms | U-72107 | ||
| Chemical Name | 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3 | ||
| Formula | C19H20N2O3S | M.Wt | 356.44 |
| Solubility | ≥ 14.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL |
| 5 mM | 561.1 μL | 2.8055 mL | 5.611 mL |
| 10 mM | 280.6 μL | 1.4028 mL | 2.8055 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)