Sitagliptin phosphate monohydrate
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Sitagliptin phosphate monohydrate
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CAS No:
654671-77-9
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Formula:
C16H15F6N5O.H3O4P.H2O
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Chemical Name:
Sitagliptin phosphate monohydrate
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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,hydrate (1:1:1);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),monohydrate;(2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine dihydrogen phosphate monohydrate;Sitagliptin phosphate monohydrate;1253056-03-9
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CAS No:
Description
Sitagliptin phosphate monohydrate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts
Sitagliptin Phosphate is the phosphate salt form of sitagliptin, an orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis.|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 monohydrate Basic Attributes
523.3240802
523.105530
1806241-263-5
TS63EW8X6F
C73811
A10BH01|A10BD24
2933990090
Safety Information
NONH for all modes of transport
28-38-41-48-62-63
24/25-26-28-36/37/39
P264, P280, P305+P351+P338, P33, P313
H319
|Warning|H319 (100%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]|P264, P280, P305+P351+P338, and P337+P313|Aggregated GHS information provided by 41 companies from 3 notifications to the ECHA C&L Inventory.
Drug Information
For adult patients with type-2 diabetes mellitus, Xelevia 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;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.Xelevia 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.|For patients with type-2 diabetes mellitus, Tesavel 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 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 witha sulphonylurea and metformin when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control;a peroxisome-proliferator-activated-receptor-gamma (PPARγ) agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control.Tesavel is also indicated as add on to insulin (with or without metformin) when diet and exercise plus stable dosage of insulin do not provide adequate glycaemic control.|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.|Steglujan is indicated in adults aged 18 years and older with type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycaemic control:when metformin and/or a sulphonylurea (SU) and one of the monocomponents of Steglujan do not provide adequate glycaemic control.in patients already being treated with the combination of ertugliflozin and sitagliptin as separate tablets.|Treatment of type II diabetes mellitus
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 monohydrate Use and Manufacturing
Sitagliptin phosphate is very effective in treating type 2 diabetes. As a new type of anti-diabetic drug, sitagliptin phosphate is blood sugar-dependent, has a moderate hypoglycemic effect, increases insulin secretion without hypoglycemia, effectively reduces hunger and other advantages, and has no nausea, vomiting, edema and increase Side effects such as body weight.
Human drugs -> Xelevia -> EMA Drug Category|Drugs used in diabetes -> Human pharmacotherapeutic group|Human drugs -> Tesavel -> EMA Drug Category|Human drugs -> Januvia -> EMA Drug Category|Human drugs -> Steglujan -> EMA Drug Category|Drugs used in diabetes, Combinations of oral blood glucose lowering drugs -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients
Computed Properties
Molecular Weight:523.32
Hydrogen Bond Donor Count:5
Hydrogen Bond Acceptor Count:15
Rotatable Bond Count:4
Exact Mass:523.10553934
Monoisotopic Mass:523.10553934
Topological Polar Surface Area:156
Heavy Atom Count:34
Complexity:616
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes
Drug Function and Efficacy
Pharmacological action not specified
Registered Holders
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CHROMO LABORATORIES INDIA PRIVATE LTD
Active
United States
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MSN LIFE SCIENCES PRIVATE LTD
Active
United States
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OPTIMUS DRUGS PRIVATE LTD
Active
United States
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Sitagliptin phosphate monohydrate
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