Peptidic dual GLP-1 / glucagon receptor agonists derived from exendin-4
A receptor and selected technology, applied in the direction of glucagon, peptide/protein components, hormone peptides, etc., can solve the chemical instability of exendin-4 and other problems
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[0420] Example 1:
[0421] Synthesize SEQ ID NO: 8
[0422] The manual synthesis method as described in the method was performed on dry Rink amide MBHA resin (0.66 mmol / g). The Fmoc-synthesis strategy is implemented with DIC / HOBt-activation. Fmoc-Lys(ivDde)-OH was used in position 14 and Boc-His(Boc)-OH was used in position 1. According to a modified literature method (S.R. Chhabra et al., Tetrahedron Lett. 39, (1998), 1603) 4% hydrazine hydrate in DMF is used to cleave the ivDde- group from the peptide on the resin. The peptide was excised from the resin with King's cocktail (D.S. King, C.G. Fields, G.B. Fields, Int. J. Peptide Protein Res. 36, 1990, 255-266). The crude product was purified via preparative HPLC using an acetonitrile / water gradient (0.1% TFA in both buffers). The purified peptide was analyzed by LCMS (Method C).
[0423] The deconvolution of the mass signal with a retention time of 12.66 minutes under the peak revealed that the peptide mass is 4557.6, which is c...
Example Embodiment
[0424] Example 2:
[0425] Synthesize SEQ ID NO: 11
[0426] The manual synthesis method as described in the method was performed on dry Rink amide MBHA resin (0.66 mmol / g). The Fmoc-synthesis strategy was implemented with DIC / HOBt-activation. Use Fmoc-Lys(ivDde)-OH in position 14 and Boc-His(Boc)-OH in position 1. According to a modified literature method (S.R. Chhabra et al., Tetrahedron Lett. 39, (1998), 1603) 4% hydrazine hydrate in DMF is used to cleave the ivDde- group from the peptide on the resin. The peptide was excised from the resin with King's cocktail (D.S. King, C.G. Fields, G.B. Fields, Int. J. Peptide Protein Res. 36, 1990, 255-266). The crude product was purified via preparative HPLC using an acetonitrile / water gradient (0.1% TFA in both buffers). The purified peptide was analyzed by LCMS (Method D).
[0427] The deconvolution of the mass signal with a retention time of 14.40 minutes under the peak revealed that the peptide mass is 4673.6, which is consistent wi...
Example Embodiment
[0435] Example 3: Stability and solubility
[0436] The solubility and stability of the peptide compound were evaluated as described in the method. The results are given in Table 5.
[0437] Table 5: Stability and solubility
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