| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
Purity: ≥98%
Pioglitazone HCl (also known as Actos; U-72107A; AD-4833; AD4833, U-72107E), the hydrochloride salt of Pioglitazone which is approved and thiazolidinedione-based anti-diabetic drug, is a selective PPARϒ agonist with hypoglycemic activity. It inhibits PPARϒ with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. It is used to treat diabetes.
| ln Vitro |
Pioglitazone added to the AGEs culture media totally reverses the effects of AGEs-induced beta cell necrosis. Moreover, pioglitazone totally stopped any increase in caspase-3 activation brought on by AGEs, bringing caspase-3 activity back to levels comparable to those of control cells. AG can, as anticipated, mitigate the reduced viability caused by AGEs[2].
|
||
|---|---|---|---|
| ln Vivo |
In ob/ob and adipo-/- ob/ob mice, serum-free fatty acid and triglyceride levels, as well as adipocyte sizes, remain unaltered following 10 mg/kg Pioglitazone administration, but are markedly decreased to a comparable extent following 30 mg/kg Pioglitazone. Additionally, after 10 mg/kg of pioglitazone, the expressions of TNFα and resistin in the adipose tissues of ob/ob and adipo-/- ob/ob mice remain unchanged, but after 30 mg/kg of pioglitazone, they drop. As a result, adiponectin may act independently in skeletal muscle and dependently in the liver during pioglitazone-induced improvement of insulin resistance and diabetes[3]. Treatment with pomiglitazone (10 mg/kg per d) effectively reduces heart hypertrophy and body weight loss. Treatment with pioglitazone dramatically lowers increased serum glucose levels and improves the dyslipidemia that is linked with it. Moreover, D rats' serum creatinine levels are marginally but significantly higher than those of their N controls (P <0.05). On the other hand, the diabetic nephropathic (DN) group shows a significant renal impairment (P<0.05). Furthermore, compared to both N and D rats, DN rats have the highest serum activity of CK-MB (P<0.05). Both increased serum levels of creatinine and creatine kinase-MB (CK-MB) can be reduced by pioglitazone[4].
|
||
| Animal Protocol |
|
||
| References |
[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 |
| Molecular Formula |
C19H20N2O3S.HCL
|
|
|---|---|---|
| Molecular Weight |
392.9
|
|
| CAS # |
112529-15-4
|
|
| Related CAS # |
Pioglitazone;111025-46-8
|
|
| SMILES |
Cl[H].S1C(N([H])C(C1([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])N=1)C([H])([H])C([H])([H])[H])=O)=O
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 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: ≥ 2.5 mg/mL (6.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5452 mL | 12.7259 mL | 25.4518 mL | |
| 5 mM | 0.5090 mL | 2.5452 mL | 5.0904 mL | |
| 10 mM | 0.2545 mL | 1.2726 mL | 2.5452 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| 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 |
| NCT01873001 | Completed | Drug: Pioglitazone HCl Drug: Abiraterone acetate |
Healthy Volunteers | Janssen Research & Development, LLC | May 2013 | Phase 1 |
| NCT02958956 | Completed Has Results | Drug: Pioglitazone | Diabetes Mellitus, Type 2, Cancer | Takeda | January 1, 1997 | |
| NCT03080480 | Terminated | Drug: Pioglitazone | Chronic Granulomatous Disease | Children's Hospital of Fudan University | September 1, 2017 | Phase 1 Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
NMR