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CAS NO.145350-09-0
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C19H21ClN2O3S |
| Molar Mass | 392.9 |
| Density | 1.329g/cm3 |
| Melting Point | 193-194°C |
| Boling Point | 666.324°C at 760 mmHg |
| Flash Point | 356.78°C |
| Water Solubility | Soluble in water (<1 mg/ml at 25°C), DMF, methanol, ethanol (4 mg/ml at 25°C), and DMSO (79 mg/ml at 25°C). |
| Solubility | DMSO : 100 mg/mL (254.52 mM; Need ultrasonic) |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White to off-white (Solid) |
| Color | white to off-white |
| Merck | 14,7452 |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.64 |
| MDL | MFCD04975446 |
| Physical and Chemical Properties | The appearance is white crystal powder, and the melting range is 193-194 ℃. |
| Use | A new generation of drugs for the treatment of type 2 diabetes |
Open Data Verified Data
research and development of the pharmaceutical industry in Koita, Japan. Approved by the U. S. Food and Drug Administration in 1999. Insulin sensitizer, for a new generation of Type II diabetes treatment drugs, side effects. It reduces insulin resistance in peripheral tissues and liver, increases insulin-dependent glucose processing, and reduces hepatic glucose output. Pioglitazone improves insulin sensitivity in patients with insulin resistance, increases insulin responsiveness to cells, and improves glucose homeostasis disorders. For the treatment of diabetes.
Last Update：2022-01-01 09:24:03
| use | pioglitazone hydrochloride can reduce insulin resistance in peripheral tissues and liver, increase insulin-dependent glucose treatment, and reduce glycogen output. It can also improve insulin sensitivity in patients with insulin resistance, increase insulin responsiveness to cells, and improve glucose balance disorders in the body. For the treatment of diabetes. A new generation of type 2 diabetes treatment drugs, side effects are small. drugs for treating diabetes |
| mechanism of action | pioglitazone and rosiglitazone are currently commonly used thiazolidinedione antidiabetic drugs in the clinical treatment of diabetes in China, and are insulin sensitizers. It can reduce insulin resistance in peripheral tissues and liver, increase the treatment of insulin-dependent glucose, and reduce the output of glycogen. The effect and mechanism of action are the same as rosiglitazone, which can reduce triglyceride (TG) and increase high density lipoprotein (HDL) during treatment. Animal experiments show that this product can reduce hyperglycemia, hyperinsulinemia and hypertriglyceride of insulin resistance. The metabolic changes caused by this product lead to an increase in insulin-dependent tissue responses. Since this product improves the effect of circulating insulin (I. e., reduces insulin resistance), it cannot reduce blood sugar in animal models lacking endogenous insulin. Pioglitazone is mainly suitable for the treatment of patients with non-insulin-dependent diabetes (type II) who cannot control blood sugar by diet and exercise alone. It can be treated alone or in combination with sulfonylurea hypoglycemic agents, metformin and insulin. |
| pharmacological effects | pioglitazone achieves lasting blood sugar control by directly reducing insulin resistance and improving β cell function. Pioglitazone is a highly selective and potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. The receptor is a protein found in adipose, skeletal and liver tissues of insulin-sensitive tissues. the absolute bioavailability of pioglitazone is 99%. after oral administration, pioglitazone can be detected in blood for 30min on an empty stomach and reach a peak concentration in 2h. Food will delay the peak concentration time to 3~4h, plasma t1/2 is 3~7h. Pioglitazone is mainly bound to serum albumin and is metabolized by hydroxylation and oxidation. Most of it is excreted into bile in the form of prototype or metabolite and cleared from feces. pioglitazone can increase insulin content in pancreatic islets but has no effect on insulin secretion. Pioglitazone prevents the reduction of β cells by reducing cell death. These evidences show that pioglitazone has a protective effect on β cells. Pioglitazone can reduce hyperinsulinemia and plasma free fatty acid levels. Decreased plasma insulin levels suggest that pioglitazone reduces the burden on pancreatic beta cells. Since the high level of free fatty acids has a toxic effect on the pancreas, reducing the level of free fatty acids also has a protective effect on the function of pancreatic β cells. Therefore, the basic physiological link of type 2 diabetes is to reduce insulin resistance, improve β cell function to control blood sugar. The above information is edited and sorted out. |
| usage and dosage | this product is treated alone. the initial dose is 15-30mg per day. it is taken before or after meals. if it is missed, it does not need to be increased, but only needs to be taken on the same day. Depending on the patient's blood sugar, the dose can be adjusted, but the maximum recommended daily dose is 45mg. Combination therapy: 1. Sulfonylurea: maintain the dosage of original sulfonylurea hypoglycemic drugs, take this product 15~30mg every day. If hypoglycemia occurs, adjust the dosage of sulfonylurea hypoglycemic drugs. 2. Metformin: Maintain the original dosage of metformin and take 15~30mg of this product every day. If hypoglycemia occurs, adjust the dosage of metformin. 3. Insulin: maintain the original insulin dosage, take this product 15~30mg every day. If hypoglycemia occurs or blood sugar drops to 100mg/dl, insulin is reduced by 10% ~ 25%. Apply this product to treat type 2 diabetes. According to the patient's hypoglycemic response, it is recommended to formulate an individualized treatment plan. For long-term treatment, HbAlC levels should be detected every three months. |
| clinical evaluation | clinical studies have shown that pioglitazone can improve insulin sensitivity in patients with insulin resistance, increase insulin responsiveness to cells, and improve glucose balance disorders in the body. The effect can last for at least 1 year. In clinical controlled trials, pioglitazone combined with sulfonylurea, metformin or insulin can improve the efficacy. Domestic multi-center, randomized, double-blind, parallel-controlled data show that pioglitazone is used for 12 weeks in patients with type 2 diabetes. The effective rate of reducing fasting blood glucose is 40.66%, the effective rate is 75.82%, and the effective rate of reducing postprandial hyperglycemia is 51.38%. The effective rate is 86.24%. After 12 weeks of application, the patient's blood pressure, heart rate, ECG and laboratory indicators were not abnormal. |
| safety | the results of a 2-year carcinogenicity test conducted in female and male rats showed that when a oral dose of pioglitazone reached 63mg/(kg d)(converted by body surface area, when equivalent to 14 times the maximum dose recommended clinically), no tumor caused by administration occurred in other organs except bladder. When the dose is ≥ 4mg/(kg d)(calculated by body surface area, almost equal to the clinically recommended maximum dose), benign and/or malignant transitional cell tumors are found in male rats. However, the results of a 2-year carcinogenicity test conducted in female and male mice showed that the oral dose reached 100mg/(kg · d)(converted by body surface area, equivalent to the maximum clinically recommended dose 11 times), no tumor caused by administration occurred in any organ. In epidemiological studies carried out abroad, the risk of bladder cancer associated with the use of pioglitazone in diabetic patients has been observed, and the risk of long-term use of pioglitazone has increased. On June 15, 2011, the FDA issued a statement informing the public that taking pioglitazone for more than 1 year may be related to the increased risk of bladder cancer. This warning message is required to be added to the label of drugs containing pioglitazone, and the patient medication guidelines for the above drugs will be revised accordingly. On June 9, 2011, the French Health, Safety and Health Products Agency (AFSSAPS) officially announced that it would suspend the sale of pioglitazone in France, along with the suspension of the sale of pioglitazone and metformin compound preparations. On June 10, 2011, the German Federal Drug and Medical Supplies Research Agency (BfArM) made the same decision as the French drug regulatory agency, suspending the sale of pioglitazone and requiring doctors not to prescribe the drug for new patients, but France and Germany Neither institution recommends that patients who are taking the drug stop taking the drug until they switch to other drugs under the guidance of a doctor. |
| precautions | patients who are allergic to this product or preparation components are prohibited. This product can only play an anti-hyperglycemic effect in the presence of insulin. Therefore, pioglitazone is not suitable for patients with type 1 diabetes or diabetic ketoacidosis. In patients with insulin resistance who have stopped ovulation before menopause, treatment with thiazolidinediones, including pioglitazone, can lead to re-ovulation. Combined with contraceptives containing ethinylestradiol and norethindrone, the plasma concentration of the two hormones can be reduced by about 30%. This product has no effect on glipizide, digoxin, warfarin and metformin. CYP3A4 inhibition has a certain effect on the metabolism of this product. Ketoconazole can obviously inhibit the metabolism of this product in vitro. No drug-induced tumors were found in other organs except the bladder. This product can increase the plasma volume, and patients with cardiac function grade III or IV should be used with caution. Liver and kidney function should be monitored during medication. |
| chemical properties | appearance is a white crystal powder with a melting range of 193-194 ℃. |
CAS:
145350-09-0
MF:
C19H20N2O4S
MW:
372.44
EINECS:
MDL No.:
MFCD00915839
Melting point:
158-160°C
Boiling point:
666.3±50.0 °C(Predicted)
Density
1.32±0.1 g/cm3(Predicted)
storage temp.
-20°C Freezer, Under Inert Atmosphere
solubility
DMSO (Slightly), Methanol (Slightly)
pka
6.34±0.50(Predicted)
form
Solid
color
White to Off-White
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.