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Sitagliptin phosphate

pharmaceutical raw materials
Sitagliptin phosphate structure

Sitagliptin phosphate 

structure
  • CAS No:

    654671-78-0

  • Formula:

    C16H15F6N5O.H3O4P

  • Chemical Name:

    Sitagliptin phosphate

  • Synonyms:

    1-Butanone,3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-,(3R)-,phosphate (1:1);1,2,4-Triazolo[4,3-a]pyrazine,7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-,phosphate (1:1);MK 0431;MK 431;Sitagliptin phosphate;Januvia;Glactiv;790712-60-6

  • Categories:

    Pharmaceutical Intermediates  >  Heterocyclic Compound

Description

White Solid


A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.

Sitagliptin phosphate Basic Attributes

505.31

505.095

494P4635I6

DTXSID10215789

A10BH01

2933990090

Characteristics

155

1.72610

white solid

215-217 °C

529.9ºC at 760 mmHg

274.3ºC

Drug Information

For adult patients with type-2 diabetes mellitus, Januvia is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a peroxisome-proliferator-activated-receptor-gamma (PPARγ) agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;a PPARγ agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination with:a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control;a PPARγ agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.Januvia is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.

Compounds that suppress the degradation of INCRETINS by blocking the action of DIPEPTIDYL-PEPTIDASE IV. This helps to correct the defective INSULIN and GLUCAGON secretion characteristic of TYPE 2 DIABETES MELLITUS by stimulating insulin secretion and suppressing glucagon release. (See all compounds classified as Dipeptidyl-Peptidase IV Inhibitors.)|Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)|Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially. (See all compounds classified as Incretins.)

0431, MK

Sitagliptin phosphate Use and Manufacturing

Uses

A trizolopyrazine dipeptidyl peptidase IV inhibitor. It has recently been approved for the therapy of type II diabetes. Sitagliptin is a trizolopyrazine dipeptidyl peptidase IV inhibitor. Sitagliptin has recently been approved for the therapy of type II diabetes.

Human drugs -> Januvia -> EMA Drug Category|Drugs used in diabetes -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:505.31
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:14
Rotatable Bond Count:4
Exact Mass:505.09497466
Monoisotopic Mass:505.09497466
Topological Polar Surface Area:155
Heavy Atom Count:33
Complexity:616
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

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