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Submit ReviewSitagliptin phosphate
Description: Potent and selective DPP IV inhibitor
Chemical Name: (3R)-3-Amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-1-butanone phosphate
Purity: ≥98% (HPLC)
Biological Activity for Sitagliptin phosphate
Sitagliptin phosphate is a potent and selective DPP IV (DPP4) inhibitor (IC50 = 18 nM). Displays >2600-fold selectivity for DPP IV over other proline specific peptidases. Reduces blood glucose and increases GLP-1 levels after oral glucose tolerance test in normal and diet-induced obese mice.
Compound Libraries for Sitagliptin phosphate
Sitagliptin phosphate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Sitagliptin phosphate
| M. Wt | 505.31 |
| Formula | C16H15F6N5O.H3O4P |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 654671-78-0 |
| PubChem ID | 6451150 |
| InChI Key | IQFYVLUXQXSJJN-SBSPUUFOSA-N |
| Smiles | OP(O)(O)=O.N[C@H](CC1=C(C=C(C(F)=C1)F)F)CC(N2CCN3C(C2)=NN=C3C(F)(F)F)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Sitagliptin phosphate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 25.27 | 50 | |
| DMSO | 25.27 | 50 |
Preparing Stock Solutions for Sitagliptin phosphate
The following data is based on the product molecular weight 505.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.96 mL | 19.79 mL | 39.58 mL |
| 2.5 mM | 0.79 mL | 3.96 mL | 7.92 mL |
| 5 mM | 0.4 mL | 1.98 mL | 3.96 mL |
| 25 mM | 0.08 mL | 0.4 mL | 0.79 mL |
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Product Datasheets for Sitagliptin phosphate
References for Sitagliptin phosphate
References are publications that support the biological activity of the product.
Kim et al (2005) (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J.Med.Chem. 48 141 PMID: 15634008
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Keywords: Sitagliptin phosphate, Sitagliptin phosphate supplier, DPPIV, DPP4, inhibitors, inhibits, potent, selective, CD26, Dipeptidyl, Peptidase, IV, (DPP-IV), 6816, Tocris Bioscience
Citations for Sitagliptin phosphate
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