CAS · 654671-78-0
Product Overview
Sitagliptin phosphate is a high-purity a-api supplied for industrial and specialty chemical applications. Contact our team for specifications, packaging options and lead times.
Product Specifications
| Property | Specification |
|---|---|
| Grade | USP41 |
| Appearance | White to off-white crystalline powder |
| Identification | HPLC, IR, PHOSPHATE |
| Assay (HPLC) | 98% to 102% |
| Bulk Density | 0.3-0.5g/ml |
| Residue on ignition | 0.2% max |
| Chiral impurity | 0.5% max |
| Water | 1.0% max |
| Related impurities | |
| Any individual impurity | 0.1% max |
| Total impurities | 0.5% max |
Applications
1. Treatment of Type 2 Diabetes Mellitus
Sitagliptin phosphate丨CAS 654671-78-0 is widely used for the management of type 2 diabetes, particularly in patients who cannot achieve adequate glycemic control with dietary changes and exercise alone.
● Monotherapy: Sitagliptin can be used as a standalone therapy in patients with type 2 diabetes who are unable to control their blood glucose levels adequately using other treatments.
● Combination Therapy: It is often used in combination with other oral antidiabetic agents like metformin, sulfonylureas, or thiazolidinediones for enhanced blood glucose control. Additionally, it can be combined with insulin therapy if required.
The drug is particularly beneficial for individuals who have a poor response to other oral hypoglycemic agents, as it improves insulin secretion and reduces hepatic glucose production without increasing the risk of hypoglycemia.
2. Adjunct to Diet and Exercise
Sitagliptin phosphate丨CAS 654671-78-0 is recommended as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes. The drug helps to maintain normal blood glucose levels by enhancing the body's own insulin production and reducing excess glucose production by the liver.
● Postprandial blood sugar control: Sitagliptin helps lower the postprandial blood sugar (the sugar level after meals), which is a common challenge for individuals with type 2 diabetes.
● Fasting blood sugar regulation: It also contributes to controlling fasting blood sugar levels, making it beneficial in overall glucose management.
3. Potential Role in Obesity Management
While not its primary indication, there is some evidence suggesting that DPP-4 inhibitors like sitagliptin may have a potential role in managing obesity and weight control in people with diabetes.
● Weight neutrality: Unlike some other diabetes medications that may cause weight gain, sitagliptin has been found to be weight-neutral, meaning it neither promotes weight loss nor gain in most patients.
● Metabolic improvement: It may improve other aspects of metabolism, including lipid profiles, as a result of better glucose control.
4. Use in Combination with SGLT-2 Inhibitors
In some cases, sitagliptin is used alongside sodium-glucose cotransporter-2 (SGLT-2) inhibitors like empagliflozin or dapagliflozin, which also treat type 2 diabetes.
● Synergistic effect: The combination works through different mechanisms to control blood glucose levels more effectively. SGLT-2 inhibitors help the kidneys excrete excess glucose, while sitagliptin enhances insulin secretion, leading to more efficient blood sugar regulation.
● Reduced cardiovascular risk: Some studies have shown that the combination may provide additional cardiovascular benefits, a significant concern for individuals with diabetes.
5. Potential Benefits in Cardiovascular Health
Although not yet fully established, some research has indicated that sitagliptin phosphate may have beneficial effects on cardiovascular health in people with diabetes. Since cardiovascular disease is a leading cause of death in type 2 diabetes patients, drugs like sitagliptin that might reduce cardiovascular risk are of significant interest.
● Blood pressure reduction: Preliminary data suggests that sitagliptin may lead to slight reductions in blood pressure, which is beneficial for diabetic patients with comorbid hypertension.
● Improved lipid profile: There is evidence suggesting that sitagliptin may improve lipid metabolism, reducing levels of harmful lipids such as triglycerides and LDL cholesterol, which contribute to heart disease risk.
Benefits
1. Improved Glycemic Control
Sitagliptin phosphate丨CAS 654671-78-0 is effective in improving glycemic control in individuals with type 2 diabetes. It works by increasing incretin levels, which promotes insulin release and reduces glucagon secretion in a glucose-dependent manner.
● Prevents postprandial hyperglycemia: Sitagliptin helps lower the blood glucose levels that spike after meals, a common challenge for those with type 2 diabetes.
● Fasting blood glucose management: The drug also plays a role in managing fasting blood glucose, a crucial element of diabetes management.
2. Low Risk of Hypoglycemia
Unlike some other diabetes medications, sitagliptin has a low risk of hypoglycemia (low blood sugar) when used alone. This makes it a safer option for many patients, as the risk of hypoglycemia can be particularly dangerous.
● Glucose-dependent mechanism: The drug only stimulates insulin release when glucose levels are elevated, reducing the risk of insulin being released when blood sugar is already low.
3. Well-Tolerated with Few Side Effects
Sitagliptin is generally well-tolerated by patients. Common side effects are typically mild and include upper respiratory tract infections, headaches, and nasal congestion. These side effects are not usually severe enough to require discontinuation of the drug.
● No major weight gain: Sitagliptin is weight-neutral, which is beneficial for many patients with type 2 diabetes who are concerned about weight gain associated with other diabetes medications.
● Minimal gastrointestinal side effects: Compared to other diabetes drugs like metformin, sitagliptin generally has fewer gastrointestinal side effects.
4. Convenient Dosing
Sitagliptin is usually taken once daily, making it a convenient option for patients who need to adhere to a medication regimen.
● Ease of use: The once-daily dosage allows for better patient compliance compared to medications that require multiple doses throughout the day.
● Flexible dosing: It can be used with or without food, further adding to the convenience for patients with busy lifestyles.
Conclusion
Sitagliptin phosphate丨CAS 654671-78-0 is a DPP-4 inhibitor widely used to treat type 2 diabetes mellitus by improving blood glucose control. It is effective both as monotherapy and in combination therapy with other diabetes medications. With its glucose-dependent mechanism of action, sitagliptin enhances insulin secretion and inhibits glucagon release, which helps regulate blood sugar levels. Its low risk of hypoglycemia, well-tolerated profile, and weight-neutral effects make it an attractive option for many patients. Additionally, ongoing research into its potential cardiovascular benefits further emphasizes its value in comprehensive diabetes management. Sitagliptin continues to be a cornerstone in the management of type 2 diabetes, improving glycemic control and offering an overall benefit to patients' health.
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