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Sitagliptin Phosphate Monohydrate CAS 654671-77-9

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  • Appearance: White powder
  • Assay: 99. 0%min
  • Stock: In stock
  • Sample: Available
  • Zhishang Chemical: Sitagliptin Phosphate Monohydrate Supplier & Manufacturer

Basic Info of Sitagliptin Phosphate Monohydrate

What is Sitagliptin Phosphate Monohydrate?

Sitagliptin phosphate (trade name Januvia, code name MK-0431) is abbreviated as sitagliptin, which is produced by Merck Company in the United States and was approved by the U.S. Food and Drug Administration (FDA) in October 2006 for the treatment of Type 2 diabetes.

The effect of sitagliptin phosphate in the therapy of type 2 diabetic issues is very satisfactory. As a brand-new type of antidiabetic medicine, sitagliptin phosphate has the advantages of blood glucose dependence, moderate hypoglycemic effect, no hypoglycemia while increasing insulin secretion, efficiently minimizing appetite, as well as no nausea, throwing up, edema and also boost Weight and opposite side results.

Sitagliptin Phosphate Monohydrate Uses

  1. Sitagliptin Phosphate Monohydrate is a dipeptidyl peptidase-IV (DPPIV) prevention that boosts the body’s very own capacity to lower excessive blood glucose levels.
  2. A pyrazine acquired dipeptidyl peptidase IV prevention and also hypoglycemic agent, which can enhance the levels of the intestinal tract insulinotropic hormone GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and also sugar dependent insulinotropic polypeptide (GIP). It is made use of to treat type 2 diabetic issues.

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Pharmacological Mechanism of Action

The existence of DPP-4 externally of T cells, called CD26, plays a crucial duty in the immune system. In addition to degrading Increlin, DPP-4 can likewise break down lots of other materials, such as growth hormone launching hormonal agent (GHRH). Neuropeptide Y, pituitary adenylate cyclization turning on peptide (PACAP).

The half-life of lncretin in vivo is very brief, it can be quickly deteriorated by DPP-4, and the tv2 of GLP-1 in plasma is ≈ 1min. There are two primary looks into on Incretin. One is to establish GLP-1 analogs that can not be broken down by DPP-4 as well as have GLP-1 task. As an example, Enaclopide, which was accepted by the US FDA in 2005, is a GLP-1 receptor agonist as well as is a subcutaneously injected polypeptide that is not conveniently weakened. The 2nd is to create inhibitors of DPP-4, as well as sitagliptin is just one of them. Sitagliptin can prevent DPP-4, increase the activity of GLP-1 and GIP in plasma, and a little raise its content, so it has a hypoglycemic impact without creating nausea or vomiting and throwing up because of excessive GLP-1 web content. Instance. Since it promotes insulin secretion with blood sugar dependancy, it can considerably reduce the incidence of hypoglycemia with dental hypoglycemic agents. On top of that, the action of sitagliptin is highly discerning. Research studies have found that its selectivity to DPP-4 is about 2600 times higher than that of DPP-8 and DPP-9, so there are couple of negative effects triggered by the inhibition of DPP-8 as well as DPP-9.

New Hypoglycemic Drug Sitagliptin Phosphate

Sitagliptin phosphate is the first dipeptidyl peptidase IV (DDP-4) inhibitor drug developed by Merck & Co. of Germany and approved by the U.S. Food and Drug Administration for the treatment of type 2 diabetes. Sugar drugs can improve the body’s own ability to reduce excessive blood sugar levels, and by inhibiting the activity of this enzyme, it can relatively increase the levels of naturally occurring incretins, including glucagon-like peptide-1 and glucose-dependent insulinotropic peptides. Trigger the clinical effect of increasing insulin production by the pancreas and stopping glucose production by the liver, ultimately lowering blood glucose concentrations. The characteristics of this product are that it can reduce hunger while stimulating insulin secretion, and will not cause weight gain, and will not cause hypoglycemia and edema. It is suitable for diabetic patients with poor blood sugar control and frequent hypoglycemia. It has been clinically verified in 552 patients with mild to moderate type 2 diabetes mellitus. Taking sitagliptin phosphate once a day, 100 mg each time, can reduce glycated hemoglobin by 0.6%-1.1% after taking the drug for 12 weeks. The incidence of adverse reactions was similar to placebo, and the most commonly reported adverse reactions (incidence >5% and higher than placebo) were nasal congestion or runny nose, as well as sore throat, upper respiratory tract infection, and headache.

Clinical studies have shown that sitagliptin phosphate as a monotherapy in patients with type 2 diabetes can significantly reduce the level of glycated hemoglobin (HbA1c). When used in combination with metformin or TZDs, it has a significant adjunctive role in targeting the three major defects of type 2 diabetes: insulin resistance, beta-cell dysfunction (reduced insulin release), and alpha-cell dysfunction (uninhibited hepatic glucose generation) to function. However, the drug should not be used for the treatment of patients with type 1 diabetes or diabetic ketoacidosis.

Sitagliptin Phosphate Monohydrate Suppliers and Manufacturers

As a sitagliptin phosphate supplier and manufacturer with strict standard product quality system certificate, Zhishang Chemical has long been providing the best sitagliptin phosphate raw materials to customers all over the world.

Over the years, relying on professional team experience and customer-centric team concept to meet customer needs in a timely manner, our company enjoys a high reputation in the world. At present, our company has served more than 6,000 customers and has established long-term cooperative relations with customers from many countries.

If you have demand for sitagliptin phosphate and related products, please contact our service staff Zhishang Chemical – White directly, we will provide you with high-quality products at the best price.

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