Sitagliptin phosphate

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Cat.No. 6816 - Sitagliptin phosphate | C16H15F6N5O.H3O4P | CAS No. 654671-78-0
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective DPP IV (DPP4) inhibitor (IC50 = 18 nM). Displays >2600-fold selectivity for DDP 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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 25.27 50
DMSO 25.27 50

Preparing Stock Solutions

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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References

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

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