Sitagliptin phosphate
- CAS No.
- 654671-78-0
- Chemical Name:
- Sitagliptin phosphate
- Synonyms
- Sitagliptin Phosphat;3-Amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]-pyrazin-7(8H)-yl)-4-(2,4,5-t;(3R)-3-aMino-1-[3-(trifluoroMethyl)-5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;SIT-11;CS-1358;sitagpliptin;Sitagliptin, MK 0431;Sitagliptin phosphate;Sitagliptin Phosphatec;Sitagliptin phosphate salt
- CBNumber:
- CB71179744
- Molecular Formula:
- C16H15F6N5O.H3PO4
- Molecular Weight:
- 505.31
- MOL File:
- 654671-78-0.mol
- Modify Date:
- 2024/4/12 23:00:59
| Melting point | 202-204°C |
|---|---|
| storage temp. | -20°C Freezer |
| solubility | Methanol (Slightly, Heated), Water (Sparingly, Sonicated) |
| form | Solid |
| color | White to Off-White |
| InChI | InChI=1S/C16H15F6N5O.H3O4P/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22;1-5(2,3)4/h4,6,9H,1-3,5,7,23H2;(H3,1,2,3,4) |
| InChIKey | IQFYVLUXQXSJJN-UHFFFAOYSA-N |
| SMILES | C(C1=CC(F)=C(F)C=C1F)C(N)CC(=O)N1CCN2C(C(F)(F)F)=NN=C2C1.P(O)(O)(O)=O |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Sitagliptin phosphate Chemical Properties,Uses,Production
Description
Sitagliptin is the first novel dipeptidyl peptidase IV inhibitor from Merck for the treatment of type 2 diabetes without weight gain and the incidence of hypoglycemia was similar to placebo. Sitagliptin acts by enhancing the body’s incretin system, which helps to regulate glucose by affecting β and α cells in the pancreas.
Chemical Properties
White Solid
Uses
A trizolopyrazine dipeptidyl peptidase IV inhibitor. It has recently been approved for the therapy of type II diabetes.
General Description
Sitagliptin phosphate is the 1:1 phosphoric acid salt ofsitagliptin free base (i.e., (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)-2-butanamine), and is marketed(Junuvia, 2006) in 25-, 50-, and 100-mg tablets. Acombination product with metformin (Janumet, 2007) intwo strengths (50 mg/500 mg and 50 mg/1,000 mgsitagliptin/metformin) is also available, and sitagliptin mayalso be prescribed with a thiazolidinedione, or possibly a sulfonylurea.The phosphate salt provides very high water solubility.The bioavailability of orally administered sitagliptinis～87%. The drug exhibits relatively low plasma protein binding (～38%), a relatively large volume of distribution(198 L), and a terminal elimination half-life of 12 hours.About 79% of a 100-mg oral dose is excreted unchanged inurine, the balance as trace-level metabolites (CYP3A4, lessercontribution by CYP2C8) in urine or feces: 87% of administeredradioactivity is excreted in urine, and 13% in feces.Active tubular excretion is reported to play a key role in renalclearance of unchanged drug, and may be mediated at least inpart via the organic anion transporter hOAT-3.
Sitagliptin phosphate Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| SURYA LIFE SCIENCES LIMITED | +91-2646226290 +91-9428511112 | Gujarat, India | 62 | 58 | Inquiry |
| ANWITA APIS | +919000311012 | Hyderabad, India | 198 | 58 | Inquiry |
| Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
| Bulat Pharmaceutical Pvt Ltd | +91-8448085659 +91-8448085660 | Haryana, India | 123 | 58 | Inquiry |
| SKVen Technologies Pvt.Ltd. | +91-7032295152 +91-7032295152 | Hyderabad, India | 81 | 58 | Inquiry |
| AARTIA KEM SCIENCE | +91-8291072530 +91-8291072530 | Maharashtra, India | 70 | 58 | Inquiry |
| Sekhment pharmaventures | +91-9030088669 +91-9030088669 | Mumbai, India | 105 | 58 | Inquiry |
| Aurobindo Pharma Limited | +914066725000 | Telangana, India | 112 | 58 | Inquiry |
| Aalidhra Pharmachem Pvt Ltd | +91-9879180894 +91-9879180894 | Gujarat, India | 38 | 58 | Inquiry |
| Honour Lab Limited | +919845977466 | Telangana, India | 164 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| SURYA LIFE SCIENCES LIMITED | 58 |
| ANWITA APIS | 58 |
| Dr. Reddy's Laboratories Ltd | 58 |
| Bulat Pharmaceutical Pvt Ltd | 58 |
| SKVen Technologies Pvt.Ltd. | 58 |
| AARTIA KEM SCIENCE | 58 |
| Sekhment pharmaventures | 58 |
| Aurobindo Pharma Limited | 58 |
| Aalidhra Pharmachem Pvt Ltd | 58 |
| Honour Lab Limited | 58 |
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