Table 1.
Physicochemical and binding properties of Ang-II and its photolabile analogues, as evaluated by competition binding assays using HEK 293-AT1 and HEK 293-AT2 transfected cells
| Binding 125I-Ang-II (HEK293-AT1R) | Binding 125I-Ang-II (HEK293-AT2R) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Compound Name | MScalc (g mol−1)* | bMSfound (g mol−1)† | Purity‡ | IC50 (nm) | pIC50 | n | IC50 (nm) | pIC50 | n |
| Ang-II | 1046.18 | 1047.10 | ≥95% | 3.2 | 8.58 ± 0.10 | 8 | 32 | 7.65 ± 0.18 | 6 |
| [Tyr(DMNB)4]Ang-II | 1241.35 | 1241.52 | ≥95% | 1110 | 6.01 ± 0.11 | 6 | 1640 | 6.88 ± 0.61 | 6 |
| Ang-II-ODMNB | 1241.35 | 1242.43 | ≥95% | 915 | 6.13 ± 0.27 | 6 | 470 | 6.45 ± 0.28 | 5 |
| [Tyr(DMNB)4]Ang-II-ODMNB | 1436.52 | 1437.52 | ≥95% | 1140 | 6.31 ± 0.27 | 6 | 1930 | 6.54 ± 0.52 | 6 |
*
Theoretical monoisotopic molecular weight as calculated with ChemDraw Ultra, version 7.0.1 (Perkin Elmer, Boston, MA, USA).
†
m/z value assessed by matrix-assisted laser desorption ionization-time of flight mass spectrometry.
‡
Percentage of purity determined by HPLC using the eluent system: A = H2O containing 0.06% TFA and B = 40% CH3CN in aqueous 0.06% TFA, with a gradient of 1% B min–1 and a flow rate of 1 ml min–1 on a Jupiter C18 column (Phenomenex). Detection at 229 nm.